Disease on EC 2.5.1.21 - squalene synthase

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DISEASE
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Acidosis
[Inhibitory action of natural compounds of microbial origin on cholesterol metabolism]
Acquired Immunodeficiency Syndrome
Successful virtual screening of a chemical database for farnesyltransferase inhibitor leads.
Acute Lung Injury
Streptococcal M1 protein triggers farnesyltransferase-dependent formation of CXC chemokines in alveolar macrophages and neutrophil infiltration in the lung.
Adenocarcinoma
A novel amplicon at 8p22-23 results in overexpression of cathepsin B in esophageal adenocarcinoma.
Enhanced Antiproliferative and Apoptotic Response of HT-29 Adenocarcinoma Cells to Combination of Photoactivated Hypericin and Farnesyltransferase Inhibitor Manumycin A.
Expression of PTEN and FHIT is involved in regulating the balance between apoptosis and proliferation in lung carcinomas.
Phase II and pharmacodynamic study of the farnesyltransferase inhibitor R115777 as initial therapy in patients with metastatic pancreatic adenocarcinoma.
The diagnostic utility of zinc E-box 1 (ZEB1) transcription factor for identification of pulmonary sarcomatoid carcinoma in cytologic and surgical specimens.
Adenoma
Effect of farnesyltransferase inhibitor FTI-276 on established lung adenomas from A/J mice induced by 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone.
Alzheimer Disease
Farnesyltransferase haplodeficiency reduces neuropathology and rescues cognitive function in a mouse model of Alzheimer disease.
Anemia
New and old treatment modalities in primary myelofibrosis.
Arrhythmias, Cardiac
Effects of sasanquasaponin on ischemia and reperfusion injury in mouse hearts.
Arthritis
Inhibition of farnesyltransferase prevents collagen-induced arthritis by down-regulation of inflammatory gene expression through suppression of p21(ras)-dependent NF-kappaB activation.
Arthritis, Experimental
Inhibition of farnesyltransferase prevents collagen-induced arthritis by down-regulation of inflammatory gene expression through suppression of p21(ras)-dependent NF-kappaB activation.
Arthritis, Rheumatoid
Dichotomous versus semi-quantitative scoring of ultrasound joint inflammation in rheumatoid arthritis using novel individualized joint selection methods.
Asthma
Exploring the potential of sequential simulation.
Farnesyltransferase Inhibition Exacerbates Eosinophilic Inflammation and Airway Hyperreactivity in Mice with Experimental Asthma: The Complex Roles of Ras GTPase and Farnesylpyrophosphate in Type 2 Allergic Inflammation.
Targeting the mevalonate cascade as a new therapeutic approach in heart disease, cancer and pulmonary disease.
Astrocytoma
Establishment and characterization of a novel malignant astrocytoma cell line derived from a tumor removed in a patient with neurofibromatosis type 1.
In vitro and in vivo growth inhibition of human malignant astrocytoma cells by the farnesyltransferase inhibitor B1620.
The farnesyltransferase inhibitor L-744,832 inhibits the growth of astrocytomas through a combination of antiproliferative, antiangiogenic, and proapoptotic activities.
Atherosclerosis
Design of more potent squalene synthase inhibitors with multiple activities.
Design of Novel Potent Antihyperlipidemic Agents with Antioxidant/Anti-inflammatory Properties: Exploiting Phenothiazine's Strong Antioxidant Activity.
Developing potential agents against atherosclerosis: Design, synthesis and pharmacological evaluation of novel dual inhibitors of oxidative stress and Squalene Synthase activity.
EP2306 [2-(4-biphenyl)-4-methyl-octahydro-1,4-benzoxazin-2-ol, hydrobromide], a novel squalene synthase inhibitor, reduces atherosclerosis in the cholesterol-fed rabbit.
Farnesyltransferase inhibitor, manumycin a, prevents atherosclerosis development and reduces oxidative stress in apolipoprotein E-deficient mice.
Therapeutic approaches to drug targets in atherosclerosis.
Brain Neoplasms
Farnesyltransferase and geranylgeranyltransferase I inhibitors upregulate RhoB expression by HDAC1 dissociation, HAT association and histone acetylation of the RhoB promoter.
Phase I and pharmacokinetic study of the oral farnesyltransferase inhibitor lonafarnib administered twice daily to pediatric patients with advanced central nervous system tumors using a modified continuous reassessment method: a Pediatric Brain Tumor Consortium Study.
Breast Neoplasms
A phase I trial and pharmacokinetic study of tipifarnib, a farnesyltransferase inhibitor, and tamoxifen in metastatic breast cancer.
A phase II trial of capecitabine in combination with the farnesyltransferase inhibitor tipifarnib in patients with anthracycline-treated and taxane-resistant metastatic breast cancer: an Eastern Cooperative Oncology Group Study (E1103).
A phase II, randomized, blinded study of the farnesyltransferase inhibitor tipifarnib combined with letrozole in the treatment of advanced breast cancer after antiestrogen therapy.
Aromatase inhibitors: combinations with fulvestrant or signal transduction inhibitors as a strategy to overcome endocrine resistance.
Biomarkers of anticancer activity of R115777 (Tipifarnib, Zarnestra) in human breast cancer models in vitro.
Combination of farnesyltransferase and Akt inhibitors is synergistic in breast cancer cells and causes significant breast tumor regression in ErbB2 transgenic mice.
Enhancement of the antitumor activity of tamoxifen and anastrozole by the farnesyltransferase inhibitor lonafarnib (SCH66336).
Experimental, Clinical and Morphological Analysis of H-Ras Oncoproteins for Locally Advanced Breast Cancer.
Farnesyltransferase inhibitors and their potential in the treatment of breast carcinoma.
Farnesyltransferase inhibitors in breast cancer therapy.
Gliotoxin is a dual inhibitor of farnesyltransferase and geranylgeranyltransferase I with antitumor activity against breast cancer in vivo.
Higenamine enhances the antitumor effects of cucurbitacin B in breast cancer by inhibiting the interaction of AKT and CDK2.
Inhibition of transendothelial migration and invasion of human breast cancer cells by preventing geranylgeranylation of Rho.
New targets for therapy in breast cancer: farnesyltransferase inhibitors.
Phase II trial of the farnesyltransferase inhibitor tipifarnib plus fulvestrant in hormone receptor-positive metastatic breast cancer: New York Cancer Consortium Trial P6205.
Potentiation of nitric oxide-induced apoptosis of MDA-MB-468 cells by farnesyltransferase inhibitor: implications in breast cancer.
Sasanquasaponin from Camellia oleifera Abel. induces cell cycle arrest and apoptosis in human breast cancer MCF-7 cells.
Targeted inhibition of farnesyltransferase in locally advanced breast cancer: a phase I and II trial of tipifarnib plus dose-dense doxorubicin and cyclophosphamide.
Targeting downstream effectors of epidermal growth factor receptor/HER2 in breast cancer with either farnesyltransferase inhibitors or mTOR antagonists.
The farnesyltransferase inhibitor R115777 (tipifarnib) in combination with tamoxifen acts synergistically to inhibit MCF-7 breast cancer cell proliferation and cell cycle progression in vitro and in vivo.
The use of molecular markers in farnesyltransferase inhibitor (FTI) therapy of breast cancer.
Tipifarnib plus tamoxifen in tamoxifen-resistant metastatic breast cancer: a negative phase II and screening of potential therapeutic markers by proteomic analysis.
Bronchiectasis
Quantitative Computed Tomography Metrics From the Transplanted Lung can Predict Forced Expiratory Volume in the First Second After Lung Transplantation.
Burkitt Lymphoma
Potent inhibition of human tumor p21ras farnesyltransferase by A1A2-lacking p21ras CA1A2X peptidomimetics.
Carcinogenesis
Functional polymorphisms in inbred rat strains and their allele frequencies in commercially available outbred stocks.
Potent farnesyltransferase inhibitor ABT-100 abrogates acute allograft rejection.
Potential biomarkers for paclitaxel sensitivity in hypopharynx cancer cell.
ras protein p21 processing enzyme farnesyltransferase in chemical carcinogen-induced murine skin tumors.
Synthesis, molecular modeling, and structure-activity relationship of benzophenone-based CAAX-peptidomimetic farnesyltransferase inhibitors.
Carcinoid Tumor
The diagnostic utility of zinc E-box 1 (ZEB1) transcription factor for identification of pulmonary sarcomatoid carcinoma in cytologic and surgical specimens.
Carcinoma
A farnesyltransferase inhibitor induces tumor regression in transgenic mice harboring multiple oncogenic mutations by mediating alterations in both cell cycle control and apoptosis.
Absence of the CAAX endoprotease Rce1: effects on cell growth and transformation.
Atorvastatin inhibits pancreatic carcinogenesis and increases survival in LSL-Kras(G12D) -LSL-Trp53(R172H) -Pdx1-Cre mice.
BAI, a novel Cdk inhibitor, enhances farnesyltransferase inhibitor LB42708-mediated apoptosis in renal carcinoma cells through the downregulation of Bcl-2 and c-FLIP (L).
Expression of PTEN and FHIT is involved in regulating the balance between apoptosis and proliferation in lung carcinomas.
Expression of the farnesyltransferase beta-subunit gene in human ovarian carcinoma: correlation to K-ras mutation.
Farnesyltransferase activity and mRNA expression in human skin basal cell carcinomas.
Farnesyltransferase inhibitor SCH-66336 downregulates secretion of matrix proteinases and inhibits carcinoma cell migration.
Farnesyltransferase inhibitor SCH66336 induces rapid phosphorylation of eukaryotic translation elongation factor 2 in head and neck squamous cell carcinoma cells.
Farnesyltransferase inhibitors--a novel approach in the treatment of advanced pancreatic carcinomas.
Inhibition of farnesyltransferase induces regression of mammary and salivary carcinomas in ras transgenic mice.
Lipid synthesis and processing proteins ABHD5, PGRMC1 and squalene synthase can serve as novel immunohistochemical markers for sebaceous neoplasms and differentiate sebaceous carcinoma from sebaceoma and basal cell carcinoma with clear cell features.
Multiple squamous cell carcinomas of the skin after therapy with sorafenib combined with tipifarnib.
Pancreatic cancer cell radiation survival and prenyltransferase inhibition: the role of K-Ras.
Phase II study of the farnesyltransferase inhibitor lonafarnib with paclitaxel in patients with taxane-refractory/resistant nonsmall cell lung carcinoma.
Potent inhibition of human tumor p21ras farnesyltransferase by A1A2-lacking p21ras CA1A2X peptidomimetics.
Suppression of rho B expression in invasive carcinoma from head and neck cancer patients.
The diagnostic utility of zinc E-box 1 (ZEB1) transcription factor for identification of pulmonary sarcomatoid carcinoma in cytologic and surgical specimens.
Carcinoma, Basal Cell
Farnesyltransferase activity and mRNA expression in human skin basal cell carcinomas.
Lipid synthesis and processing proteins ABHD5, PGRMC1 and squalene synthase can serve as novel immunohistochemical markers for sebaceous neoplasms and differentiate sebaceous carcinoma from sebaceoma and basal cell carcinoma with clear cell features.
Carcinoma, Hepatocellular
A Link between cholesterol levels and phenobarbital induction of cytochromes P450.
ATF6? Stimulates Cholesterogenic Gene Expression and de Novo Cholesterol Synthesis.
Pravastatin inhibited the cholesterol synthesis in human hepatoma cell line Hep G2 less than simvastatin and lovastatin, which is reflected in the upregulation of 3-hydroxy-3-methylglutaryl coenzyme A reductase and squalene synthase.
Rational Discovery of Novel Squalene Synthase Inhibitors through Pharmacophore Modelling.
Regulation of squalene synthetase in human hepatoma cell line Hep G2 by sterols, and not by mevalonate-derived non-sterols.
Sasanquasaponin from Camellia oleifera Abel. induces cell cycle arrest and apoptosis in human breast cancer MCF-7 cells.
Subcellular localization of squalene synthase in human hepatoma cell line Hep G2.
Syntheses and biological evaluation of novel quinuclidine derivatives as squalene synthase inhibitors.
Syntheses of 3-ethylidenequinuclidine derivatives as squalene synthase inhibitors. Part 2: enzyme inhibition and effects on plasma lipid levels.
Targeting Cellular Squalene Synthase, an Enzyme Essential for Cholesterol Biosynthesis, Is a Potential Antiviral Strategy against Hepatitis C Virus.
[Correlation between inhibitory effect of Manumycin on human hepatoma cancer cell HepG2 and Ras signal transduction pathway]
Carcinoma, Large Cell
Expression of PTEN and FHIT is involved in regulating the balance between apoptosis and proliferation in lung carcinomas.
The diagnostic utility of zinc E-box 1 (ZEB1) transcription factor for identification of pulmonary sarcomatoid carcinoma in cytologic and surgical specimens.
Carcinoma, Neuroendocrine
The diagnostic utility of zinc E-box 1 (ZEB1) transcription factor for identification of pulmonary sarcomatoid carcinoma in cytologic and surgical specimens.
Carcinoma, Non-Small-Cell Lung
Farnesyltransferase inhibitors as radiation sensitizers.
In vitro study of farnesyltransferase inhibitor SCH 66336, in combination with chemotherapy and radiation, in non-small cell lung cancer cell lines.
Ras homologue enriched in brain is a critical target of farnesyltransferase inhibitors in non-small cell lung cancer cells.
Relationship of SNP rs2645429 in Farnesyl-Diphosphate Farnesyltransferase 1 Gene Promoter with Susceptibility to Lung Cancer.
Carcinoma, Renal Cell
Multiple squamous cell carcinomas of the skin after therapy with sorafenib combined with tipifarnib.
Carcinoma, Small Cell
Expression of PTEN and FHIT is involved in regulating the balance between apoptosis and proliferation in lung carcinomas.
Carcinoma, Squamous Cell
Farnesyltransferase inhibitor SCH66336 induces rapid phosphorylation of eukaryotic translation elongation factor 2 in head and neck squamous cell carcinoma cells.
The diagnostic utility of zinc E-box 1 (ZEB1) transcription factor for identification of pulmonary sarcomatoid carcinoma in cytologic and surgical specimens.
Cardiovascular Diseases
A farnesyltransferase inhibitor prevents both the onset and late progression of cardiovascular disease in a progeria mouse model.
Squalene synthase: a critical enzyme in the cholesterol biosynthesis pathway.
Successful virtual screening of a chemical database for farnesyltransferase inhibitor leads.
Targeting the mevalonate cascade as a new therapeutic approach in heart disease, cancer and pulmonary disease.
Cataract
Lanosterol synthase mutations cause cholesterol deficiency-associated cataracts in the Shumiya cataract rat.
Lens cholesterol biosynthesis inhibition: A common mechanism of cataract formation in laboratory animals by pharmaceutical products.
Cell Transformation, Neoplastic
Biotherapeutic approaches to pancreatic cancer.
Pancreatic cancer: a review of emerging therapies.
Central Nervous System Neoplasms
Phase I and pharmacokinetic study of the oral farnesyltransferase inhibitor lonafarnib administered twice daily to pediatric patients with advanced central nervous system tumors using a modified continuous reassessment method: a Pediatric Brain Tumor Consortium Study.
Chagas Disease
Biphenylquinuclidines as inhibitors of squalene synthase and growth of parasitic protozoa.
In vitro and in vivo activities of E5700 and ER-119884, two novel orally active squalene synthase inhibitors, against Trypanosoma cruzi.
Squalene synthase as a target for Chagas disease therapeutics.
Chondrodysplasia Punctata
Genetic disorders of cholesterol biosynthesis in mice and humans.
Colonic Neoplasms
Cellular effects of a new farnesyltransferase inhibitor, RPR-115135, in a human isogenic colon cancer cell line model system HCT-116.
In vitro and in vivo evaluation of two rational-designed nonpeptidic farnesyltransferase inhibitors on HT29 human colon cancer cell lines.
Induction of micronuclei by a new non-peptidic mimetic farnesyltransferase inhibitor RPR-115135: role of gene mutations.
Liver metastasis models of colon cancer for evaluation of drug efficacy using NOD/Shi-scid IL2Rgammanull (NOG) mice.
Nonpeptidomimetic farnesyltransferase inhibitor RPR-115135 increases cytotoxicity of 5-fluorouracil: role of p53.
RPR-115135, a farnesyltransferase inhibitor, increases 5-FU- cytotoxicity in ten human colon cancer cell lines: role of p53.
RPR-115135, a new non peptidomimetic farnesyltransferase inhibitor, induces G0/G1 arrest only in serum starved cells.
Colorectal Neoplasms
A significant role of lipogenic enzymes in colorectal cancer.
Biochemical changes of mevalonate pathway in human colorectal cancer.
Increased farnesyltransferase activity in human colorectal cancer: relationship with clinicopathological features and K-ras mutation.
Inhibition of the mitogen-activated protein kinase pathway results in the down-regulation of P-glycoprotein.
Oncogenic K-Ras signals through epidermal growth factor receptor and wild-type H-Ras to promote radiation survival in pancreatic and colorectal carcinoma cells.
Coronary Artery Disease
Lapaquistat acetate, a squalene synthase inhibitor, changes macrophage/lipid-rich coronary plaques of hypercholesterolaemic rabbits into fibrous lesions.
Craniosynostoses
Additional squamosal suture synostosis and segmented intracranial volume in patients with non-syndromic sagittal synostosis.
Diphtheria
Update in childhood acute myeloid leukemia: recent developments in the molecular basis of disease and novel therapies.
Dyslipidemias
Design of Novel Potent Antihyperlipidemic Agents with Antioxidant/Anti-inflammatory Properties: Exploiting Phenothiazine's Strong Antioxidant Activity.
Squalene synthase inhibition: a novel target for the management of dyslipidemia.
Endotoxemia
Farnesyltransferase inhibitor improved survival following endotoxin challenge in mice.
Erythema
Exclusion of CTSB and FDFT1 as positional and functional candidate genes for keratolytic winter erythema (KWE).
Exanthema
L-NAME has opposite effects on the productions of S-adenosylhomocysteine and S-adenosylmethionine in V12-H-Ras and M-CR3B-Ras pheochromocytoma cells.
Glioblastoma
?v?3 Integrin and Fibroblast growth factor receptor 1 (FGFR1): Prognostic factors in a phase I-II clinical trial associating continuous administration of Tipifarnib with radiotherapy for patients with newly diagnosed glioblastoma.
HDJ-2 as a target for radiosensitization of glioblastoma multiforme cells by the farnesyltransferase inhibitor R115777 and the role of the p53/p21 pathway.
Inhibition of cell growth in human glioblastoma cell lines by farnesyltransferase inhibitor SCH66336.
Inhibition of Farnesyltransferase Potentiates NOTCH-Targeted Therapy against Glioblastoma Stem Cells.
The farnesyltransferase inhibitor R115777 reduces hypoxia and matrix metalloproteinase 2 expression in human glioma xenograft.
Glioma
Farnesyltransferase Inhibitor Manumycin Targets IL1?-Ras-HIF-1? Axis in Tumor Cells of Diverse Origin.
Farnesyltransferase inhibitor, R115777, reverses the resistance of human glioma cell lines to ionizing radiation.
Farnesyltransferase inhibitors: promises and realities.
Inhibition of Ras and related guanosine triphosphate-dependent proteins as a therapeutic strategy for blocking malignant glioma growth: II--preclinical studies in a nude mouse model.
Lonafarnib (SCH66336) improves the activity of temozolomide and radiation for orthotopic malignant gliomas.
Manumycin inhibits STAT3, telomerase activity and growth of glioma cells by elevating intracellular reactive oxygen species generation.
Phase 1/1b study of lonafarnib and temozolomide in patients with recurrent or temozolomide refractory glioblastoma.
Phase I trial of tipifarnib in children with newly diagnosed intrinsic diffuse brainstem glioma.
Phase I trial of tipifarnib in patients with recurrent malignant glioma taking enzyme-inducing antiepileptic drugs: a North American Brain Tumor Consortium Study.
Phase II trial of tipifarnib and radiation in children with newly diagnosed diffuse intrinsic pontine gliomas.
Phase II trial of tipifarnib in patients with recurrent malignant glioma either receiving or not receiving enzyme-inducing antiepileptic drugs: a North American Brain Tumor Consortium Study.
Selective inhibition of cholesterol biosynthesis in brain cells by squalestatin 1.
TGF-?-induced hCG-? regulates redox homeostasis in glioma cells.
The farnesyltransferase inhibitor R115777 reduces hypoxia and matrix metalloproteinase 2 expression in human glioma xenograft.
Glomerulonephritis
Functional polymorphisms in inbred rat strains and their allele frequencies in commercially available outbred stocks.
Head and Neck Neoplasms
A Phase I trial of the farnesyltransferase inhibitor L-778,123 and radiotherapy for locally advanced lung and head and neck cancer.
Farnesyltransferase inhibitors as radiation sensitizers.
Hematologic Neoplasms
Clinical activity of tipifarnib in hematologic malignancies.
Clinical development of farnesyltransferase inhibitors in leukemias and myelodysplastic syndrome.
Continuous and intermittent dosing of lonafarnib potentiates the therapeutic efficacy of docetaxel on preclinical human prostate cancer models.
Development of farnesyltransferase inhibitors for clinical cancer therapy: focus on hematologic malignancies.
Development of the farnesyltransferase inhibitor tipifarnib for therapy of hematologic malignancies.
Farnesyltransferase inhibition in hematologic malignancies: the clinical experience with tipifarnib.
Farnesyltransferase inhibitors in hematologic malignancies: new horizons in therapy.
Farnesyltransferase inhibitors: novel compounds in development for the treatment of myeloid malignancies.
Farnesyltransferase inhibitors: where are we now?
Farnesyltransferase inihibitors in hematologic malignancies.
Future clinical implications for farnesyltransferase inhibitors in hematologic malignancies.
In Vitro Apoptotic Effects of Farnesyltransferase blockade in Acute Myeloid Leukemia Cells.
Myelodysplastic syndrome overview.
Role of farnesyltransferase inhibitors in hematologic malignancies.
Tipifarnib and tanespimycin show synergic proapoptotic activity in U937 cells.
Hepatitis C
Farnesyl-diphosphate farnesyltransferase 1 regulates hepatitis C virus propagation.
Targeting Cellular Squalene Synthase, an Enzyme Essential for Cholesterol Biosynthesis, Is a Potential Antiviral Strategy against Hepatitis C Virus.
Hepatitis C, Chronic
Role of FDFT1 polymorphism for fibrosis progression in patients with chronic hepatitis C.
Hepatitis D, Chronic
Current and Future Management of Chronic Hepatitis D.
Hyperalgesia
Differential Effects of Subcutaneous Electrical Stimulation (SQS) and Transcutaneous Electrical Nerve Stimulation (TENS) in Rodent Models of Chronic Neuropathic or Inflammatory Pain.
Hypercholesterolemia
Antiproliferative and ultrastructural effects of BPQ-OH, a specific inhibitor of squalene synthase, on Leishmania amazonensis.
Increased cholesterol biosynthesis and hypercholesterolemia in mice overexpressing squalene synthase in the liver.
Isolation and structural determination of squalene synthase inhibitor from Prunus mume fruit.
Lapaquistat acetate: development of a squalene synthase inhibitor for the treatment of hypercholesterolemia.
Lead nitrate-induced development of hypercholesterolemia in rats: sterol-independent gene regulation of hepatic enzymes responsible for cholesterol homeostasis.
Pharmacologic inhibition of squalene synthase and other downstream enzymes of the cholesterol synthesis pathway: a new therapeutic approach to treatment of hypercholesterolemia.
Potential role of nonstatin cholesterol lowering agents.
Squalene synthase: a critical enzyme in the cholesterol biosynthesis pathway.
Hyperinsulinism
Effect of insulin on farnesyltransferase gene transcription and mRNA stability.
Fetal hyperinsulinemia increases farnesylation of p21 Ras in fetal tissues.
Hyperinsulinemia potentiates activation of p21Ras by growth factors.
Insulin potentiates platelet-derived growth factor action in vascular smooth muscle cells.
Mechanism of the mitogenic influence of hyperinsulinemia.
Hyperlactatemia
Burn-induced muscle metabolic derangements and mitochondrial dysfunction are associated with activation of HIF-1? and mTORC1: Role of protein farnesylation.
Hyperlipidemias
Characteristics of the squalene synthase inhibitors produced by a Streptomyces species isolated from soils.
Cholesterol diet-induced hyperlipidemia influences gene expression pattern of rat hearts: a DNA microarray study.
Design of Novel Potent Antihyperlipidemic Agents with Antioxidant/Anti-inflammatory Properties: Exploiting Phenothiazine's Strong Antioxidant Activity.
Discovery of Potential Inhibitors of Squalene Synthase from Traditional Chinese Medicine Based on Virtual Screening and In Vitro Evaluation of Lipid-Lowering Effect.
Docking study of novel antihyperlipidemic thieno[2,3-d]pyrimidine; LM-1554, with some molecular targets related to hyperlipidemia - an investigation into its mechanism of action.
Drug evaluation: TAK-475--an oral inhibitor of squalene synthase for hyperlipidemia.
Evaluation of potential inhibitors of squalene synthase based on virtual screening and in vitro studies.
Hyperlipoproteinemia Type II
Lipid-lowering effects of TAK-475, a squalene synthase inhibitor, in animal models of familial hypercholesterolemia.
Hyperpigmentation
Automated in vivo screen in zebrafish identifies Clotrimazole as targeting a metabolic vulnerability in a melanoma model.
Hypersensitivity
Differential Effects of Subcutaneous Electrical Stimulation (SQS) and Transcutaneous Electrical Nerve Stimulation (TENS) in Rodent Models of Chronic Neuropathic or Inflammatory Pain.
Hypersensitivity of abscisic acid-induced cytosolic calcium increases in the Arabidopsis farnesyltransferase mutant era1-2.
Role of farnesyltransferase in ABA regulation of guard cell anion channels and plant water loss.
Squalene is lipotoxic to yeast cells defective in lipid droplet biogenesis.
Hypertension, Pulmonary
Effect of limonene and sobrerol on monocrotaline-induced lung alterations and pulmonary hypertension.
Tipifarnib prevents development of hypoxia-induced pulmonary hypertension.
Hypertrophy, Right Ventricular
Effect of limonene and sobrerol on monocrotaline-induced lung alterations and pulmonary hypertension.
Infections
Endotoxin, tumor necrosis factor, and interleukin-1 decrease hepatic squalene synthase activity, protein, and mRNA levels in Syrian hamsters.
Expression, purification, and characterization of the human squalene synthase: use of yeast and baculoviral systems.
Farnesyl-diphosphate farnesyltransferase 1 regulates hepatitis C virus propagation.
Lonafarnib synergizes with azoles against Aspergillus spp. and Exophiala spp.
Quantitative Proteomic Analysis of Simian Primary Hepatocytes Reveals Candidate Molecular Markers for Permissiveness to Relapsing Malaria Plasmodium Cynomolgi.
The farnesyltransferase ?-subunit RAM1 regulates localization of RAS proteins and appressorium-mediated infection in Magnaporthe oryzae.
Insulin Resistance
Burn-induced muscle metabolic derangements and mitochondrial dysfunction are associated with activation of HIF-1? and mTORC1: Role of protein farnesylation.
Mechanism of the mitogenic influence of hyperinsulinemia.
Mitogenic action of insulin: friend, foe or 'frenemy'?
Role of protein farnesylation in burn-induced metabolic derangements and insulin resistance in mouse skeletal muscle.
The Association Between Hepatic Fat Content and Liver Injury in Obese Children and Adolescents: Effects of ethnicity, insulin resistance, and common gene variants.
Kidney Failure, Chronic
Farnesyltransferase inhibitor R115777 protects against vascular disease in uremic mice.
Leishmaniasis
Biphenylquinuclidines as inhibitors of squalene synthase and growth of parasitic protozoa.
Leukemia
A phase I clinical-pharmacodynamic study of the farnesyltransferase inhibitor tipifarnib in combination with the proteasome inhibitor bortezomib in advanced acute leukemias.
Advancing the treatment of hematologic malignancies through the development of targeted interventions.
Clinical and biologic activity of the farnesyltransferase inhibitor R115777 in adults with refractory and relapsed acute leukemias: a phase 1 clinical-laboratory correlative trial.
Clinical development of farnesyltransferase inhibitors in leukemias and myelodysplastic syndrome.
Clinical improvement by farnesyltransferase inhibition in NK large granular lymphocyte leukemia associated with imbalanced NK receptor signaling.
Combination of tipifarnib and rapamycin synergistically inhibits the growth of leukemia cells and overcomes resistance to tipifarnib via alteration of cellular signaling pathways.
Complete remission following clofarabine treatment in refractory juvenile myelomonocytic leukemia.
Current status of clinical trials of farnesyltransferase inhibitors.
Enhancement of manumycin A-induced apoptosis by methoxyamine in myeloid leukemia cells.
Farnesyltransferase inhibitors and myeloid malignancies: phase I evidence of Zarnestra activity in high-risk leukemias.
Farnesyltransferase inhibitors interact synergistically with the Chk1 inhibitor UCN-01 to induce apoptosis in human leukemia cells through interruption of both Akt and MEK/ERK pathways and activation of SEK1/JNK.
Farnesyltransferase inhibitors: promises and realities.
Inhibition of juvenile myelomonocytic leukemia cell growth in vitro by farnesyltransferase inhibitors.
Low-Dose Farnesyltransferase Inhibitor Suppresses HIF-1? and Snail Expression in Triple-Negative Breast Cancer MDA-MB-231 Cells In Vitro.
Novel targeted drug therapies for the treatment of childhood acute leukemia.
Relative importance of apoptosis and cell cycle blockage in the synergistic effect of combined R115777 and imatinib treatment in BCR/ABL-positive cell lines.
Role of farnesyltransferase inhibitors in hematologic malignancies.
Sasanquasaponin from Camellia oleifera Abel. induces cell cycle arrest and apoptosis in human breast cancer MCF-7 cells.
Leukemia, Large Granular Lymphocytic
Clinical improvement by farnesyltransferase inhibition in NK large granular lymphocyte leukemia associated with imbalanced NK receptor signaling.
Tipifarnib-mediated suppression of T-bet-dependent signaling pathways.
Leukemia, Lymphocytic, Chronic, B-Cell
Farnesyltransferase inhibitor BMS-214662 induces apoptosis in B-cell chronic lymphocytic leukemia cells.
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Chronic myeloid leukemia: current therapies and the potential role of farnesyltransferase inhibitors.
Cloning and characterization of a human BCR/ABL-positive cell line, K562/RR, resistant to the farnesyltransferase inhibition by tipifarnib.
Involvement of nitric oxide in farnesyltransferase inhibitor-mediated apoptosis in chronic myeloid leukemia cells.
Leukemia, Myeloid
Combination of tipifarnib and rapamycin synergistically inhibits the growth of leukemia cells and overcomes resistance to tipifarnib via alteration of cellular signaling pathways.
In vitro and in vivo effects of a farnesyltransferase inhibitor on Nf1-deficient hematopoietic cells.
Synergistic cytotoxic effects in myeloid leukemia cells upon cotreatment with farnesyltransferase and geranylgeranyl transferase-I inhibitors.
Leukemia, Myeloid, Acute
A 2-gene classifier for predicting response to the farnesyltransferase inhibitor tipifarnib in acute myeloid leukemia.
A phase 1-2 study of a farnesyltransferase inhibitor, tipifarnib, combined with idarubicin and cytarabine for patients with newly diagnosed acute myeloid leukemia and high-risk myelodysplastic syndrome.
A phase 2 study of the farnesyltransferase inhibitor tipifarnib in poor-risk and elderly patients with previously untreated acute myelogenous leukemia.
A phase 2 study of the oral farnesyltransferase inhibitor tipifarnib in patients with refractory or relapsed acute myeloid leukemia.
Active oral regimen for elderly adults with newly diagnosed acute myelogenous leukemia: a preclinical and phase 1 trial of the farnesyltransferase inhibitor tipifarnib (R115777, Zarnestra) combined with etoposide.
Combining simvastatin with the farnesyltransferase inhibitor tipifarnib results in an enhanced cytotoxic effect in a subset of primary CD34+ acute myeloid leukemia samples.
Farnesyltransferase inhibitor therapy in acute myelogenous leukemia.
Farnesyltransferase inhibitor tipifarnib inhibits Rheb prenylation and stabilizes Bax in acute myelogenous leukemia cells.
Farnesyltransferase inhibitors in acute myeloid leukemia and myelodysplastic syndromes.
Four different regimens of farnesyltransferase inhibitor tipifarnib in older, untreated acute myeloid leukemia patients: North American Intergroup Phase II study SWOG S0432.
Identification of molecular predictors of response in a study of tipifarnib treatment in relapsed and refractory acute myelogenous leukemia.
In vitro antiproliferative activity of the farnesyltransferase inhibitor R115777 in hematopoietic progenitors from patients with myelofibrosis with myeloid metaplasia.
In Vitro Apoptotic Effects of Farnesyltransferase blockade in Acute Myeloid Leukemia Cells.
Role of farnesyltransferase inhibitors in hematologic malignancies.
Suppression of farnesyltransferase activity in acute myeloid leukemia and myelodysplastic syndrome: current understanding and recommended use of tipifarnib.
[Farnesyltransferase inhibitors: preliminary results in acute myeloid leukemia]
Leukemia, Myelomonocytic, Juvenile
Inhibition of juvenile myelomonocytic leukemia cell growth in vitro by farnesyltransferase inhibitors.
Lipodystrophy
Farnesyltransferase inhibitors prevent HIV protease inhibitor (lopinavir/ritonavir)-induced lipodystrophy and metabolic syndrome in mice.
Liver Diseases
Association of polymorphisms in GCKR and TRIB1 with nonalcoholic fatty liver disease and metabolic syndrome traits.
Plasma cholesterol-lowering and transient liver dysfunction in mice lacking squalene synthase in the liver.
Liver Failure, Acute
Farnesyltransferase inhibitor, tipifarnib, prevents galactosamine/lipopolysaccharide-induced acute liver failure.
Liver Neoplasms
Expression of farnesyltransferase in primary liver cancer.
Farnesyltransferase inhibitor, ABT-100, is a potent liver cancer chemopreventive agent.
Growth inhibition by the farnesyltransferase inhibitor FTI-277 involves Bcl-2 expression and defective association with Raf-1 in liver cancer cell lines.
Lung Diseases
Targeting the mevalonate cascade as a new therapeutic approach in heart disease, cancer and pulmonary disease.
Lung Injury
Effect of limonene and sobrerol on monocrotaline-induced lung alterations and pulmonary hypertension.
Lung Neoplasms
An overview of farnesyltransferase inhibitors and their role in lung cancer therapy.
Combined p21-activated kinase and farnesyltransferase inhibitor treatment exhibits enhanced anti-proliferative activity on melanoma, colon and lung cancer cell lines.
Correlation between high salt intake and mortality rates for oesophageal and gastric cancers in Henan Province, China.
Effects of insulin-like growth factor binding protein-3 and farnesyltransferase inhibitor SCH66336 on Akt expression and apoptosis in non-small-cell lung cancer cells.
Farnesyltransferase inhibitors are potent lung cancer chemopreventive agents in A/J mice with a dominant-negative p53 and/or heterozygous deletion of Ink4a/Arf.
Farnesyltransferase inhibitors as radiation sensitizers.
Farnesyltransferase inhibitors: promises and realities.
Hypoxia-inducible factor 1alpha and antiangiogenic activity of farnesyltransferase inhibitor SCH66336 in human aerodigestive tract cancer.
In vitro study of farnesyltransferase inhibitor SCH 66336, in combination with chemotherapy and radiation, in non-small cell lung cancer cell lines.
Ras homologue enriched in brain is a critical target of farnesyltransferase inhibitors in non-small cell lung cancer cells.
Relationship of SNP rs2645429 in Farnesyl-Diphosphate Farnesyltransferase 1 Gene Promoter with Susceptibility to Lung Cancer.
Squalene synthase induces tumor necrosis factor receptor 1 enrichment in lipid rafts to promote lung cancer metastasis.
The farnesyltransferase inhibitor Lonafarnib induces growth arrest or apoptosis of human lung cancer cells without downregulation of Akt.
The farnesyltransferase inhibitor R115777 up-regulates the expression of death receptor 5 and enhances TRAIL-induced apoptosis in human lung cancer cells.
The farnesyltransferase inhibitor, FTI-2153, blocks bipolar spindle formation and chromosome alignment and causes prometaphase accumulation during mitosis of human lung cancer cells.
The farnesyltransferase inhibitor, FTI-2153, inhibits bipolar spindle formation during mitosis independently of transformation and Ras and p53 mutation status.
The role of farnesyltransferase inhibitors in lung cancer therapy.
Lymphoma
Farnesyltransferase inhibitor R115777 inhibits cell growth and induces apoptosis in mantle cell lymphoma.
Farnesyltransferase inhibitor tipifarnib inhibits Rheb prenylation and stabilizes Bax in acute myelogenous leukemia cells.
Multi-institutional phase II of the farnesyltransferase inhibitor tipifarnib (R115777) in patients with relapsed and refractory lymphomas.
Phase II trial and prediction of response of single agent tipifarnib in patients with relapsed/refractory mantle cell lymphoma: a Groupe d'Etude des Lymphomes de l'Adulte trial.
Lymphoma, B-Cell
Phase II trial and prediction of response of single agent tipifarnib in patients with relapsed/refractory mantle cell lymphoma: a Groupe d'Etude des Lymphomes de l'Adulte trial.
Lymphoma, Mantle-Cell
Farnesyltransferase inhibitor R115777 inhibits cell growth and induces apoptosis in mantle cell lymphoma.
Phase II trial and prediction of response of single agent tipifarnib in patients with relapsed/refractory mantle cell lymphoma: a Groupe d'Etude des Lymphomes de l'Adulte trial.
Malaria
2-Oxotetrahydroquinoline-based antimalarials with high potency and metabolic stability.
Development of benzophenone-based farnesyltransferase inhibitors as novel antimalarials.
Effect of Farnesyltransferase Inhibitor R115777 on Mitochondria of Plasmodium falciparum.
Farnesyltransferase inhibitors inhibit the growth of malaria parasites in vitro and in vivo.
Molecular dynamic simulations and structure-based pharmacophore development for farnesyltransferase inhibitors discovery.
Potent, Plasmodium-selective farnesyltransferase inhibitors that arrest the growth of malaria parasites: structure-activity relationships of ethylenediamine-analogue scaffolds and homology model validation.
Structurally simple farnesyltransferase inhibitors arrest the growth of malaria parasites.
Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites.
The Recent Development of Farnesyltransferase Inhibitors as Anticancer and Antimalarial Agents.
Melanoma
Activated N-ras contributes to the chemoresistance of human melanoma in severe combined immunodeficiency (SCID) mice by blocking apoptosis.
Combined p21-activated kinase and farnesyltransferase inhibitor treatment exhibits enhanced anti-proliferative activity on melanoma, colon and lung cancer cell lines.
Phase II study of the farnesyltransferase inhibitor R115777 in advanced melanoma (CALGB 500104).
Sasanquasaponin ??? from Schima crenata Korth induces autophagy through Akt/mTOR/p70S6K pathway and promotes apoptosis in human melanoma A375 cells.
Mesothelioma
Farnesyltransferase inhibitors and human malignant pleural mesothelioma: a first-step comparative translational study.
Metabolic Syndrome
Farnesyltransferase inhibitors prevent HIV protease inhibitor (lopinavir/ritonavir)-induced lipodystrophy and metabolic syndrome in mice.
Metabolism, Inborn Errors
Genetic disorders of cholesterol biosynthesis in mice and humans.
Mevalonate Kinase Deficiency
Anti-inflammatory and cytoprotective effects of a squalene synthase inhibitor, TAK-475 active metabolite-I, in immune cells simulating mevalonate kinase deficiency (MKD)-like condition.
Genetic disorders of cholesterol biosynthesis in mice and humans.
Multiple Myeloma
Farnesyltransferase inhibitor R115777 (Zarnestra, Tipifarnib) synergizes with paclitaxel to induce apoptosis and mitotic arrest and to inhibit tumor growth of multiple myeloma cells.
Farnesyltransferase inhibitor tipifarnib is well tolerated, induces stabilization of disease, and inhibits farnesylation and oncogenic/tumor survival pathways in patients with advanced multiple myeloma.
Farnesyltransferase inhibitors and rapamycin in the treatment of multiple myeloma.
Farnesyltransferase inhibitors and their role in the treatment of multiple myeloma.
The farnesyltransferase inhibitor L744832 potentiates UCN-01-induced apoptosis in human multiple myeloma cells.
Muscular Diseases
Protective effects of a squalene synthase inhibitor, lapaquistat acetate (TAK-475), on statin-induced myotoxicity in guinea pigs.
Mycoses
Synthetic arylquinuclidine derivatives exhibit antifungal activity against Candida albicans, Candida tropicalis and Candida parapsilopsis.
Virus-induced gene silencing of Withania somnifera squalene synthase negatively regulates sterol and defence-related genes resulting in reduced withanolides and biotic stress tolerance.
Myelodysplastic Syndromes
A multicenter phase 2 study of the farnesyltransferase inhibitor tipifarnib in intermediate- to high-risk myelodysplastic syndrome.
A phase 1-2 study of a farnesyltransferase inhibitor, tipifarnib, combined with idarubicin and cytarabine for patients with newly diagnosed acute myeloid leukemia and high-risk myelodysplastic syndrome.
Advancing the treatment of hematologic malignancies through the development of targeted interventions.
Clinical development of farnesyltransferase inhibitors in leukemias and myelodysplastic syndrome.
Farnesyltransferase inhibitor R115777 in myelodysplastic syndrome: clinical and biologic activities in the phase 1 setting.
Farnesyltransferase inhibitors and their potential role in therapy for myelodysplastic syndromes and acute myeloid leukaemia.
Farnesyltransferase inhibitors in acute myeloid leukemia and myelodysplastic syndromes.
Farnesyltransferase inhibitors in myelodysplastic syndrome.
In vitro effects of the farnesyltransferase inhibitor tipifarnib on myelodysplastic syndrome progenitors.
Suppression of farnesyltransferase activity in acute myeloid leukemia and myelodysplastic syndrome: current understanding and recommended use of tipifarnib.
Myocardial Infarction
Lapaquistat acetate, a squalene synthase inhibitor, changes macrophage/lipid-rich coronary plaques of hypercholesterolaemic rabbits into fibrous lesions.
Neurologic features of Hutchinson-Gilford progeria syndrome after lonafarnib treatment.
[Evaluation of ventricular arrhythmias late after coronary artery bypass graft surgery--relation to clinical variables]
Myotoxicity
Discovery of Potential Inhibitors of Squalene Synthase from Traditional Chinese Medicine Based on Virtual Screening and In Vitro Evaluation of Lipid-Lowering Effect.
Inhibition of cholesterol synthesis by squalene synthase inhibitors does not induce myotoxicity in vitro.
Protective effects of a squalene synthase inhibitor, lapaquistat acetate (TAK-475), on statin-induced myotoxicity in guinea pigs.
Statins induce apoptosis in rat and human myotube cultures by inhibiting protein geranylgeranylation but not ubiquinone.
Neoplasm Metastasis
Biotherapeutic approaches to pancreatic cancer.
Feasibility of CT scan-guided Tru-Cut serial liver biopsies to evaluate pharmacodynamic endpoints in patients with liver metastasis treated with experimental drugs.
Liver metastasis models of colon cancer for evaluation of drug efficacy using NOD/Shi-scid IL2Rgammanull (NOG) mice.
Novel anticancer targets and drug discovery in post genomic age.
Pancreatic cancer: a review of emerging therapies.
Selective inhibition of cancer cell invasion by a geranylgeranyltransferase-I inhibitor.
Squalene synthase induces tumor necrosis factor receptor 1 enrichment in lipid rafts to promote lung cancer metastasis.
Neoplasms
(--)-Xanthatin selectively induces GADD45? and stimulates caspase-independent cell death in human breast cancer MDA-MB-231 cells.
3D-QSAR with the aid of pharmacophore search and docking-based alignments for farnesyltransferase inhibitors.
8-Hydroxyquinoline-based inhibitors of the Rce1 protease disrupt Ras membrane localization in human cells.
A farnesyltransferase inhibitor induces tumor regression in transgenic mice harboring multiple oncogenic mutations by mediating alterations in both cell cycle control and apoptosis.
A highly potent and selective farnesyltransferase inhibitor ABT-100 in preclinical studies.
A novel amplicon at 8p22-23 results in overexpression of cathepsin B in esophageal adenocarcinoma.
A phase I open label study of the farnesyltransferase inhibitor CP-609,754 in patients with advanced malignant tumors.
A phase I study of the farnesyltransferase inhibitor Tipifarnib in combination with the epidermal growth factor tyrosine kinase inhibitor Erlotinib in patients with advanced solid tumors.
A phase I, pharmacokinetic, and biological study of the farnesyltransferase inhibitor tipifarnib in combination with gemcitabine in patients with advanced malignancies.
Absence of the CAAX endoprotease Rce1: effects on cell growth and transformation.
Activity of SCH 66336, a tricyclic farnesyltransferase inhibitor, against human tumor colony-forming units.
Advances in the development of farnesyltransferase inhibitors: substrate recognition by protein farnesyltransferase.
Advancing the treatment of hematologic malignancies through the development of targeted interventions.
Androgen-dependent alternative mRNA isoform expression in prostate cancer cells.
Anticancer Activity of BIM-46174, a New Inhibitor of the Heterotrimeric G{alpha}/G{beta}{gamma} Protein Complex.
Antitumor effect of a farnesyl protein transferase inhibitor in mammary and lymphoid tumors overexpressing N-ras in transgenic mice.
Apoptotic and cytostatic farnesyltransferase inhibitors have distinct pharmacology and efficacy profiles in tumor models.
Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency.
Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.
Assessment of the bioactive conformation of the farnesyltransferase protein binding recognition motif by computational methods.
Atorvastatin inhibits pancreatic carcinogenesis and increases survival in LSL-Kras(G12D) -LSL-Trp53(R172H) -Pdx1-Cre mice.
Autophagy induced by farnesyltransferase inhibitors in cancer cells.
Biochemical changes of mevalonate pathway in human colorectal cancer.
Biotherapeutic approaches to pancreatic cancer.
BMS-214662 potently induces apoptosis of chronic myeloid leukemia stem and progenitor cells and synergizes with tyrosine kinase inhibitors.
Both farnesylated and geranylgeranylated RhoB inhibit malignant transformation and suppress human tumor growth in nude mice.
Both farnesyltransferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic K-Ras prenylation but each alone is sufficient to suppress human tumor growth in nude mouse xenografts.
c-myc down-regulation induces apoptosis in human cancer cell lines exposed to RPR-115135 (C31H29NO4), a non-peptidomimetic farnesyltransferase inhibitor.
Cdk inhibitors, roscovitine and olomoucine, synergize with farnesyltransferase inhibitor (FTI) to induce efficient apoptosis of human cancer cell lines.
Characterization of farnesyl diphosphate farnesyl transferase 1 (FDFT1) expression in cancer.
Chemoprevention of benzo(a)pyrene-induced lung tumors in mice by the farnesyltransferase inhibitor R115777.
Chemopreventive effect of perillyl alcohol on 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone induced tumorigenesis in (C3H/HeJ X A/J)F1 mouse lung.
Chemopreventive efficacy of promising farnesyltransferase inhibitors.
Clinical and pharmacologic study of the farnesyltransferase inhibitor tipifarnib in cancer patients with normal or mildly or moderately impaired hepatic function.
Combined effect of protein kinase B inhibitor or extracellular signal-regulated kinase inhibitor against farnesyltransferase inhibition-induced apoptosis in SiHa cells.
Combined p21-activated kinase and farnesyltransferase inhibitor treatment exhibits enhanced anti-proliferative activity on melanoma, colon and lung cancer cell lines.
Combining the farnesyltransferase inhibitor lonafarnib with paclitaxel results in enhanced growth inhibitory effects on human ovarian cancer models in vitro and in vivo.
Comparison of Multiparametric MRI Scoring Systems and the Impact on Cancer Detection in Patients Undergoing MR US Fusion Guided Prostate Biopsies.
Computational Enzymatic Catalysis.
Computer-aided drug design and ADMET predictions for identification and evaluation of novel potential farnesyltransferase inhibitors in cancer therapy.
Continuous and intermittent dosing of lonafarnib potentiates the therapeutic efficacy of docetaxel on preclinical human prostate cancer models.
Correlation between high salt intake and mortality rates for oesophageal and gastric cancers in Henan Province, China.
Current status of clinical trials of farnesyltransferase inhibitors.
Development of farnesyltransferase inhibitors for clinical cancer therapy: focus on hematologic malignancies.
Effect of farnesyltransferase inhibitor FTI-276 on established lung adenomas from A/J mice induced by 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone.
Effect of novel CAAX peptidomimetic farnesyltransferase inhibitor on angiogenesis in vitro and in vivo.
Effects of statins and farnesyltransferase inhibitors on the development and progression of cancer.
Efficacy of the farnesyltransferase inhibitor R115777 in a rat mammary tumor model: role of Ha-ras mutations and use of microarray analysis in identifying potential targets.
Endotoxin, tumor necrosis factor, and interleukin-1 decrease hepatic squalene synthase activity, protein, and mRNA levels in Syrian hamsters.
Enhancement of interleukin-12 gene-based tumor immunotherapy by the reduced secretion of p40 subunit and the combination with farnesyltransferase inhibitor.
Enhancement of tumor response by farnesyltransferase inhibitor in C3H/HeJ hepatocarcinoma.
Enlarging the scope of cell-penetrating prenylated peptides to include farnesylated 'CAAX' box sequences and diverse cell types.
Evolving therapies: farnesyltransferase inhibitors.
Expression of farnesyltransferase in primary liver cancer.
Expression of the farnesyltransferase beta-subunit gene in human ovarian carcinoma: correlation to K-ras mutation.
Farnesylated proteins and cell cycle progression.
Farnesyltransferase and geranylgeranyltransferase I inhibitors and cancer therapy: lessons from mechanism and bench-to-bedside translational studies.
Farnesyltransferase and geranylgeranyltransferase I inhibitors in cancer therapy: important mechanistic and bench to bedside issues.
Farnesyltransferase and geranylgeranyltransferase I inhibitors upregulate RhoB expression by HDAC1 dissociation, HAT association and histone acetylation of the RhoB promoter.
Farnesyltransferase and geranylgeranyltransferase I: structures, mechanism, inhibitors and molecular modeling.
Farnesyltransferase inhibition in hematologic malignancies: the clinical experience with tipifarnib.
Farnesyltransferase inhibitor effects on prostate tumor micro-environment and radiation survival.
Farnesyltransferase inhibitor FTI-277 inhibits PD-L1 expression on septic spleen lymphocytes and promotes spleen lymphocyte activation.
Farnesyltransferase Inhibitor Manumycin Targets IL1?-Ras-HIF-1? Axis in Tumor Cells of Diverse Origin.
Farnesyltransferase inhibitor R115777 (Zarnestra, Tipifarnib) synergizes with paclitaxel to induce apoptosis and mitotic arrest and to inhibit tumor growth of multiple myeloma cells.
Farnesyltransferase inhibitor R115777 inhibits cell growth and induces apoptosis in mantle cell lymphoma.
Farnesyltransferase inhibitor SCH66336 induces rapid phosphorylation of eukaryotic translation elongation factor 2 in head and neck squamous cell carcinoma cells.
Farnesyltransferase inhibitor therapy in acute myelogenous leukemia.
Farnesyltransferase inhibitor, ABT-100, is a potent liver cancer chemopreventive agent.
Farnesyltransferase inhibitor-induced regression of mammary tumors in TGF alpha and TGF alpha/neu transgenic mice correlates with inhibition of map kinase and p70s6 kinase phosphorylation.
Farnesyltransferase inhibitors (FTIs) in myeloid malignancies.
Farnesyltransferase inhibitors and cancer treatment: targeting simply Ras?
Farnesyltransferase inhibitors and human malignant pleural mesothelioma: a first-step comparative translational study.
Farnesyltransferase inhibitors and myeloid malignancies: phase I evidence of Zarnestra activity in high-risk leukemias.
Farnesyltransferase inhibitors as anticancer agents: current status.
Farnesyltransferase inhibitors as radiation sensitizers.
Farnesyltransferase inhibitors in myelodysplastic syndrome.
Farnesyltransferase inhibitors induce cytochrome c release and caspase 3 activation preferentially in transformed cells.
Farnesyltransferase inhibitors induce DNA damage via reactive oxygen species in human cancer cells.
Farnesyltransferase inhibitors induce dramatic morphological changes of KNRK cells that are blocked by microtubule interfering agents.
Farnesyltransferase inhibitors potentiate the antitumor effect of radiation on a human tumor xenograft expressing activated HRAS.
Farnesyltransferase inhibitors reverse Ras-mediated inhibition of Fas gene expression.
Farnesyltransferase inhibitors target multiple endothelial cell functions in angiogenesis.
Farnesyltransferase inhibitors.
Farnesyltransferase Inhibitors: A Comprehensive Review Based on Quantitative Structural Analysis.
Farnesyltransferase inhibitors: a new class of cancer chemotherapeutics.
Farnesyltransferase inhibitors: a promising future in cancer treatment.
Farnesyltransferase inhibitors: antineoplastic mechanism and clinical prospects.
Farnesyltransferase inhibitors: antineoplastic properties, mechanisms of action, and clinical prospects.
Farnesyltransferase inhibitors: novel compounds in development for the treatment of myeloid malignancies.
Farnesyltransferase inhibitors: potential role in the treatment of cancer.
Farnesyltransferase inhibitors: Ras research yields a potential cancer therapeutic.
Farnesyltransferase inhibitors: targeting the molecular basis of cancer.
Geranylgeranylated RhoB mediates suppression of human tumor cell growth by farnesyltransferase inhibitors.
Geranylgeranyltransferase I inhibitor GGTI-2154 induces breast carcinoma apoptosis and tumor regression in H-Ras transgenic mice.
GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells.
Growth inhibition by the farnesyltransferase inhibitor FTI-277 involves Bcl-2 expression and defective association with Raf-1 in liver cancer cell lines.
High affinity for farnesyltransferase and alternative prenylation contribute individually to K-Ras4B resistance to farnesyltransferase inhibitors.
Hypoxia-inducible factor 1alpha and antiangiogenic activity of farnesyltransferase inhibitor SCH66336 in human aerodigestive tract cancer.
Identification of novel peptide substrates for protein farnesyltransferase reveals two substrate classes with distinct sequence selectivities.
Implications of farnesyltransferase and its inhibitors as a promising strategy for cancer therapy.
In vitro and in vivo effects of a farnesyltransferase inhibitor on Nf1-deficient hematopoietic cells.
Increased farnesyltransferase activity in human colorectal cancer: relationship with clinicopathological features and K-ras mutation.
Induction of N-myc in neuroblastoma by autocrine IGF-II depends on farnesylated Ras. Application of farnesyltransferase inhibitors.
Inhibiting Ras signaling in the therapy of breast cancer.
Inhibition of farnesyltransferase increases TGFbeta type II receptor expression and enhances the responsiveness of human cancer cells to TGFbeta.
Inhibition of farnesyltransferase reduces angiogenesis by interrupting endothelial cell migration.
Inhibition of farnesyltransferase with A-176120, a novel and potent farnesyl pyrophosphate analogue.
Inhibition of human tumor cell growth in vitro and in vivo by a specific inhibitor of human farnesyltransferase: BIM-46068.
Inhibition of human tumor cell growth in vivo by an orally bioavailable inhibitor of human farnesyltransferase, BIM-46228.
Inhibition of Ras and related guanosine triphosphate-dependent proteins as a therapeutic strategy for blocking malignant glioma growth: II--preclinical studies in a nude mouse model.
Inhibition of the prenylation of K-Ras, but not H- or N-Ras, is highly resistant to CAAX peptidomimetics and requires both a farnesyltransferase and a geranylgeranyltransferase I inhibitor in human tumor cell lines.
Inhibition of the Ras/Raf/MEK/ERK and RET Kinase Pathways with the Combination of the Multikinase Inhibitor Sorafenib and the Farnesyltransferase Inhibitor Tipifarnib in Medullary and Differentiated Thyroid Malignancies.
Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?
Lipid synthesis and processing proteins ABHD5, PGRMC1 and squalene synthase can serve as novel immunohistochemical markers for sebaceous neoplasms and differentiate sebaceous carcinoma from sebaceoma and basal cell carcinoma with clear cell features.
Lonafarnib (SCH66336) improves the activity of temozolomide and radiation for orthotopic malignant gliomas.
Low-Dose Farnesyltransferase Inhibitor Suppresses HIF-1? and Snail Expression in Triple-Negative Breast Cancer MDA-MB-231 Cells In Vitro.
Manumycin induces apoptosis in human hepatocellular carcinoma HepG2 cells.
MicroRNA induction by copy number gain is associated with poor outcome in squamous cell carcinoma of the lung.
Molecular dynamic simulations and structure-based pharmacophore development for farnesyltransferase inhibitors discovery.
Molecular Pathways: Targeting the Dependence of Mutant RAS Cancers on the DNA Damage Response.
New tricks for human farnesyltransferase inhibitor: cancer and beyond.
Non-Ras targets of farnesyltransferase inhibitors: focus on Rho.
Novel anticancer targets and drug discovery in post genomic age.
Novel approaches to target pancreatic cancer.
Pancreatic cancer cell radiation survival and prenyltransferase inhibition: the role of K-Ras.
Pancreatic cancer: a review of emerging therapies.
Phase I and pharmacokinetic study of the farnesyltransferase inhibitor R115777 in combination with irinotecan in patients with advanced cancer.
Phase I and pharmacokinetic study of the oral farnesyltransferase inhibitor lonafarnib administered twice daily to pediatric patients with advanced central nervous system tumors using a modified continuous reassessment method: a Pediatric Brain Tumor Consortium Study.
Phase I and pharmacological study of the farnesyltransferase inhibitor tipifarnib (Zarnestra, R115777) in combination with gemcitabine and cisplatin in patients with advanced solid tumours.
Phase I and pharmacological study of the oral farnesyltransferase inhibitor SCH 66336 given once daily to patients with advanced solid tumours.
Phase I clinical trial of the farnesyltransferase inhibitor BMS-214662 administered as a weekly 24 h continuous intravenous infusion in patients with advanced solid tumors.
Phase I clinical trial of the farnesyltransferase inhibitor BMS-214662 given as a 1-hour intravenous infusion in patients with advanced solid tumors.
Phase I pharmacokinetic and pharmacodynamic study of weekly 1-hour and 24-hour infusion BMS-214662, a farnesyltransferase inhibitor, in patients with advanced solid tumors.
Phase I study of the farnesyltransferase inhibitor BMS-214662 given weekly in patients with solid tumors.
Phase I study of the farnesyltransferase inhibitor lonafarnib with paclitaxel in solid tumors.
Phase I study of the farnesyltransferase inhibitor lonafarnib with weekly paclitaxel in patients with solid tumors.
Phase I trial and pharmacokinetic study of the farnesyltransferase inhibitor tipifarnib in children with refractory solid tumors or neurofibromatosis type I and plexiform neurofibromas.
Phase I trial of a combination of the multikinase inhibitor sorafenib and the farnesyltransferase inhibitor tipifarnib in advanced malignancies.
Phase II trial of the farnesyltransferase inhibitor tipifarnib plus fulvestrant in hormone receptor-positive metastatic breast cancer: New York Cancer Consortium Trial P6205.
Post-translational modifications and regulation of the RAS superfamily of GTPases as anticancer targets.
Potent inhibition of human tumor p21ras farnesyltransferase by A1A2-lacking p21ras CA1A2X peptidomimetics.
Potentiated antitumor effects of a combination therapy with a farnesyltransferase inhibitor L-744,832 and butyrate in vitro.
Potentiation of nitric oxide-induced apoptosis of MDA-MB-468 cells by farnesyltransferase inhibitor: implications in breast cancer.
Probing the hydrophobic pocket of farnesyltransferase: aromatic substitution of CAAX peptidomimetics leads to highly potent inhibitors.
Protein farnesylation in mammalian cells: effects of farnesyltransferase inhibitors on cancer cells.
Pyridone-containing farnesyltransferase inhibitors: synthesis and biological evaluation.
Quantitative Gene Expression of ERG9 in Model Saccharomyces cerevisiae: Chamomile Extract For Human Cancer Treatment.
R115777 (Zarnestra)/Zoledronic acid (Zometa) cooperation on inhibition of prostate cancer proliferation is paralleled by Erk/Akt inactivation and reduced Bcl-2 and bad phosphorylation.
Radiation sensitization by inhibition of activated Ras.
Ras CAAX peptidomimetic FTI 276 selectively blocks tumor growth in nude mice of a human lung carcinoma with K-Ras mutation and p53 deletion.
Ras farnesyltransferase inhibitors suppress the phenotype resulting from an activated ras mutation in Caenorhabditis elegans.
Ras processing as a therapeutic target in hematologic malignancies.
ras protein p21 processing enzyme farnesyltransferase in chemical carcinogen-induced murine skin tumors.
Reactive oxygen species-dependent destruction of MEK and Akt in Manumycin stimulated death of lymphoid tumor and myeloma cell lines.
Recent advances in understanding the antineoplastic mechanisms of farnesyltransferase inhibitors.
RhoB, not RhoA, represses the transcription of the transforming growth factor beta type II receptor by a mechanism involving activator protein 1.
Role of squalene synthase in prostate cancer risk and the biological aggressiveness of human prostate cancer.
Sasanquasaponin from Camellia oleifera Abel. induces cell cycle arrest and apoptosis in human breast cancer MCF-7 cells.
Selective inhibition of cancer cell invasion by a geranylgeranyltransferase-I inhibitor.
Sequential simulation (SqS) of clinical pathways: a tool for public and patient engagement in point-of-care diagnostics.
Squalene synthase induces tumor necrosis factor receptor 1 enrichment in lipid rafts to promote lung cancer metastasis.
Squalene synthase, a determinant of Raft-associated cholesterol and modulator of cancer cell proliferation.
Stimulating Effect of Manumycin A on Suicidal Erythrocyte Death.
Successful molecular dynamics simulation of the zinc-bound farnesyltransferase using the cationic dummy atom approach.
Successful virtual screening of a chemical database for farnesyltransferase inhibitor leads.
Synthesis and anti-migrative evaluation of moverastin derivatives.
Synthesis, biodistribution and effects of farnesyltransferase inhibitor therapy on tumour uptake in mice of 99mTc labelled epidermal growth factor.
Synthesis, molecular modeling, and structure-activity relationship of benzophenone-based CAAX-peptidomimetic farnesyltransferase inhibitors.
Targeted inhibition of farnesyltransferase in locally advanced breast cancer: a phase I and II trial of tipifarnib plus dose-dense doxorubicin and cyclophosphamide.
Targeting farnesyltransferase: is Ras relevant?
Targeting the mevalonate cascade as a new therapeutic approach in heart disease, cancer and pulmonary disease.
Targeting the Ras signaling pathway: a rational, mechanism-based treatment for hematologic malignancies?
The diagnostic utility of zinc E-box 1 (ZEB1) transcription factor for identification of pulmonary sarcomatoid carcinoma in cytologic and surgical specimens.
The discovery of a novel compound with potent antitumor activity: virtual screening, synthesis, biological evaluation and preliminary mechanism study.
The farnesyl transferase inhibitor RPR-130401 does not alter radiation susceptibility in human tumor cells with a K-Ras mutation in spite of large changes in ploidy and lamin B distribution.
The farnesyl transferase inhibitor, FTI-277, inhibits growth and induces apoptosis in drug-resistant myeloma tumor cells.
The farnesyltransferase inhibitor L744,832 reduces hypoxia in tumors expressing activated H-ras.
The Farnesyltransferase Inhibitor LB42708 Suppresses VEGF-induced Angiogenesis by Inhibiting Ras-dependent MAPK and PI3K/Akt Signal Pathways.
The farnesyltransferase inhibitor lonafarnib induces CCAAT/enhancer-binding protein homologous protein-dependent expression of death receptor 5, leading to induction of apoptosis in human cancer cells.
The farnesyltransferase inhibitor R115777 up-regulates the expression of death receptor 5 and enhances TRAIL-induced apoptosis in human lung cancer cells.
The farnesyltransferase inhibitor, FPT inhibitor III upregulates Bax and Bcl-xs expression and induces apoptosis in human ovarian cancer cells.
The geranylgeranyltransferase-I inhibitor GGTI-298 arrests human tumor cells in G0/G1 and induces p21(WAF1/CIP1/SDI1) in a p53-independent manner.
The noncoding RNAs SNORD50A and SNORD50B bind K-Ras and are recurrently deleted in human cancer.
The potential of farnesyltransferase inhibitors as cancer chemotherapeutics.
The Recent Development of Farnesyltransferase Inhibitors as Anticancer and Antimalarial Agents.
Therapeutic targets in radiotherapy.
Towards complete sets of farnesylated and geranylgeranylated proteins.
Translational control and cancer therapy.
Tumorigenic activity and therapeutic inhibition of Rheb GTPase.
Unraveling the mechanism of the farnesyltransferase enzyme.
Use of synthetic isoprenoids to target protein prenylation and Rho GTPases in breast cancer invasion.
Virtual lead identification of farnesyltransferase inhibitors based on ligand and structure-based pharmacophore techniques.
[Farnesyltransferase as target for non-cytotoxic anti-cancer agents: first steps]
[Inhibitors of farnesyltransferase: a new approach for development of potential cancer drugs]
Neuralgia
Differential Effects of Subcutaneous Electrical Stimulation (SQS) and Transcutaneous Electrical Nerve Stimulation (TENS) in Rodent Models of Chronic Neuropathic or Inflammatory Pain.
Neuroblastoma
24S-hydroxycholesterol effects on lipid metabolism genes are modeled in traumatic brain injury.
Farnesyltransferase inhibitor attenuates methamphetamine toxicity-induced Ras proteins activation and cell death in neuroblastoma SH-SY5Y cells.
Farnesyltransferase inhibitor FTI-277 prevents autocrine growth stimulation of neuroblastoma by BDNF.
Induction of N-myc in neuroblastoma by autocrine IGF-II depends on farnesylated Ras. Application of farnesyltransferase inhibitors.
Neurofibroma, Plexiform
Phase 2 randomized, flexible crossover, double-blinded, placebo-controlled trial of the farnesyltransferase inhibitor tipifarnib in children and young adults with neurofibromatosis type 1 and progressive plexiform neurofibromas.
Phase I trial and pharmacokinetic study of the farnesyltransferase inhibitor tipifarnib in children with refractory solid tumors or neurofibromatosis type I and plexiform neurofibromas.
Neurofibromatoses
Farnesyltransferase inhibitors block the neurofibromatosis type I (NF1) malignant phenotype.
Phase 2 randomized, flexible crossover, double-blinded, placebo-controlled trial of the farnesyltransferase inhibitor tipifarnib in children and young adults with neurofibromatosis type 1 and progressive plexiform neurofibromas.
Phase I trial and pharmacokinetic study of the farnesyltransferase inhibitor tipifarnib in children with refractory solid tumors or neurofibromatosis type I and plexiform neurofibromas.
Neurofibromatosis 1
Farnesyltransferase inhibitors block the neurofibromatosis type I (NF1) malignant phenotype.
Phase 2 randomized, flexible crossover, double-blinded, placebo-controlled trial of the farnesyltransferase inhibitor tipifarnib in children and young adults with neurofibromatosis type 1 and progressive plexiform neurofibromas.
Phase I trial and pharmacokinetic study of the farnesyltransferase inhibitor tipifarnib in children with refractory solid tumors or neurofibromatosis type I and plexiform neurofibromas.
Non-alcoholic Fatty Liver Disease
Association of polymorphisms in GCKR and TRIB1 with nonalcoholic fatty liver disease and metabolic syndrome traits.
Association Study of Seven GWAS-Identified Common Variants with Nonalcoholic Fatty Liver Disease in Chinese Children.
The Epidemiology, Risk Profiling and Diagnostic Challenges of Nonalcoholic Fatty Liver Disease.
Obesity
Biological stereoselectivity of atropisomeric natural products and drugs.
Studies of CTNNBL1 and FDFT1 variants and measures of obesity: analyses of quantitative traits and case-control studies in 18,014 Danes.
Obesity, Morbid
Studies of CTNNBL1 and FDFT1 variants and measures of obesity: analyses of quantitative traits and case-control studies in 18,014 Danes.
Osteosarcoma
Driven to Death: Inhibition of Farnesylation Increases Ras Activity in Osteosarcoma and Promotes Growth Arrest and Cell Death.
Ovarian Neoplasms
Combining the farnesyltransferase inhibitor lonafarnib with paclitaxel results in enhanced growth inhibitory effects on human ovarian cancer models in vitro and in vivo.
Involvement of caspase family proteases in FPT inhibitor III-induced apoptosis in human ovarian cancer cells.
Randomized phase II trial of carboplatin and paclitaxel with or without lonafarnib in first-line treatment of epithelial ovarian cancer stage IIB-IV.
The farnesyltransferase inhibitor, FPT inhibitor III upregulates Bax and Bcl-xs expression and induces apoptosis in human ovarian cancer cells.
Pancreatic Neoplasms
A phase I trial of the dual farnesyltransferase and geranylgeranyltransferase inhibitor L-778,123 and radiotherapy for locally advanced pancreatic cancer.
Farnesyltransferase inhibitor (L-744,832) restores TGF-beta type II receptor expression and enhances radiation sensitivity in K-ras mutant pancreatic cancer cell line MIA PaCa-2.
Inhibition of growth and invasive activity of human pancreatic cancer cells by a farnesyltransferase inhibitor, manumycin.
Nanoformulation of Geranylgeranyltransferase-I Inhibitors for Cancer Therapy: Liposomal Encapsulation and pH-Dependent Delivery to Cancer Cells.
Novel approaches to target pancreatic cancer.
Phase III trial of gemcitabine plus tipifarnib compared with gemcitabine plus placebo in advanced pancreatic cancer.
Requirement of c-jun N-terminal kinase for apoptotic cell death induced by farnesyltransferase inhibitor, farnesylamine, in human pancreatic cancer cells.
[Oleylamine (long-chain fatty amine)-induced cell death through MAP kinase pathways in human pancreatic cancer cells]
Pancreatitis
Farnesyltransferase regulates neutrophil recruitment and tissue damage in acute pancreatitis.
Papilloma
ras protein p21 processing enzyme farnesyltransferase in chemical carcinogen-induced murine skin tumors.
Parasitic Diseases
Biphenylquinuclidines as inhibitors of squalene synthase and growth of parasitic protozoa.
Pheochromocytoma
L-NAME has opposite effects on the productions of S-adenosylhomocysteine and S-adenosylmethionine in V12-H-Ras and M-CR3B-Ras pheochromocytoma cells.
Pneumonia
Streptococcal M1 protein triggers farnesyltransferase-dependent formation of CXC chemokines in alveolar macrophages and neutrophil infiltration in the lung.
Polycythemia Vera
Farnesyltransferase inhibitor tipifarnib (R115777) preferentially inhibits in vitro autonomous erythropoiesis of polycythemia vera patient cells.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Environment-mediated drug resistance in Bcr/Abl-positive acute lymphoblastic leukemia.
Farnesyltransferase inhibitors: molecular evidence of therapeutic efficacy in acute lymphoblastic leukemia through cyclin d1 inhibition.
Increased resistance to a farnesyltransferase inhibitor by N-cadherin expression in Bcr/Abl-P190 lymphoblastic leukemia cells.
Resistance to farnesyltransferase inhibitors in Bcr/Abl-positive lymphoblastic leukemia by increased expression of a novel ABC transporter homolog ATP11a.
Primary Myelofibrosis
In vitro antiproliferative activity of the farnesyltransferase inhibitor R115777 in hematopoietic progenitors from patients with myelofibrosis with myeloid metaplasia.
Progeria
A farnesyltransferase inhibitor improves disease phenotypes in mice with a Hutchinson-Gilford progeria syndrome mutation.
A farnesyltransferase inhibitor prevents both the onset and late progression of cardiovascular disease in a progeria mouse model.
Clinical trial of a farnesyltransferase inhibitor in children with Hutchinson-Gilford progeria syndrome.
Defective lamin A-Rb signaling in Hutchinson-Gilford Progeria Syndrome and reversal by farnesyltransferase inhibition.
Disruption of lamin B1 and lamin B2 processing and localization by farnesyltransferase inhibitors.
Dynamics of lamin-A processing following precursor accumulation.
Dysfunction of iPSC-derived endothelial cells in human Hutchinson-Gilford progeria syndrome.
Farnesyltransferase inhibitor and rapamycin correct aberrant genome organisation and decrease DNA damage respectively, in Hutchinson-Gilford progeria syndrome fibroblasts.
Farnesyltransferase inhibitor treatment restores chromosome territory positions and active chromosome dynamics in Hutchinson-Gilford Progeria syndrome cells.
Incomplete processing of mutant lamin A in Hutchinson-Gilford progeria leads to nuclear abnormalities, which are reversed by farnesyltransferase inhibition.
Increased mechanosensitivity and nuclear stiffness in Hutchinson-Gilford progeria cells: effects of farnesyltransferase inhibitors.
Intermittent treatment with farnesyltransferase inhibitor and sulforaphane improves cellular homeostasis in Hutchinson-Gilford progeria fibroblasts.
Molecular dynamic simulations and structure-based pharmacophore development for farnesyltransferase inhibitors discovery.
Neurologic features of Hutchinson-Gilford progeria syndrome after lonafarnib treatment.
Progeria, the nucleolus and farnesyltransferase inhibitors.
Treatment with a farnesyltransferase inhibitor improves survival in mice with a Hutchinson-Gilford progeria syndrome mutation.
Prostatic Diseases
Role of squalene synthase in prostate cancer risk and the biological aggressiveness of human prostate cancer.
Prostatic Neoplasms
Androgen-dependent alternative mRNA isoform expression in prostate cancer cells.
Comparison of Multiparametric MRI Scoring Systems and the Impact on Cancer Detection in Patients Undergoing MR US Fusion Guided Prostate Biopsies.
Potent Farnesyltransferase Inhibitors with 1,4-Diazepane Scaffolds as Novel Destabilizing Microtubule Agents in Hormone-Resistant Prostate Cancer.
Role of squalene synthase in prostate cancer risk and the biological aggressiveness of human prostate cancer.
Squalene synthase, a determinant of Raft-associated cholesterol and modulator of cancer cell proliferation.
Pulmonary Disease, Chronic Obstructive
Targeting the mevalonate cascade as a new therapeutic approach in heart disease, cancer and pulmonary disease.
Sepsis
Farnesyltransferase inhibitor FTI-277 inhibits PD-L1 expression on septic spleen lymphocytes and promotes spleen lymphocyte activation.
Farnesyltransferase inhibitor, FTI-277, reduces mortality of septic mice along with improved bacterial clearance.
Sexually Transmitted Diseases
Aromatase inhibitors: combinations with fulvestrant or signal transduction inhibitors as a strategy to overcome endocrine resistance.
Sleep Initiation and Maintenance Disorders
A New Single-Item Sleep Quality Scale: Results of Psychometric Evaluation in Patients With Chronic Primary Insomnia and Depression.
squalene synthase deficiency
Basis for abnormal desquamation and permeability barrier dysfunction in RXLI.
Squalene Synthase Deficiency: Clinical, Biochemical, and Molecular Characterization of a Defect in Cholesterol Biosynthesis.
Squamous Cell Carcinoma of Head and Neck
Farnesyltransferase inhibitor SCH66336 induces rapid phosphorylation of eukaryotic translation elongation factor 2 in head and neck squamous cell carcinoma cells.
Stomach Neoplasms
Correlation between high salt intake and mortality rates for oesophageal and gastric cancers in Henan Province, China.
Streptococcal Infections
Streptococcal M1 protein triggers farnesyltransferase-dependent formation of CXC chemokines in alveolar macrophages and neutrophil infiltration in the lung.
Stroke
Neurologic features of Hutchinson-Gilford progeria syndrome after lonafarnib treatment.
Synostosis
Additional squamosal suture synostosis and segmented intracranial volume in patients with non-syndromic sagittal synostosis.
The Significance of Squamosal Suture Synostosis.
Synovitis
Analysis of correlation and causes for discrepancy between quantitative and semi-quantitative Doppler scores in synovitis in rheumatoid arthritis.
Tauopathies
A farnesyltransferase inhibitor activates lysosomes and reduces tau pathology in mice with tauopathy.
Thyroid Carcinoma, Anaplastic
Angiogenesis inhibition in the in vivo antineoplastic effect of manumycin and paclitaxel against anaplastic thyroid carcinoma.
Bcl-2-associated X protein is the main mediator of manumycin a-induced apoptosis in anaplastic thyroid cancer cells.
Combining a matrix metalloproteinase inhibitor, a farnesyltransferase inhibitor, and a taxane improves survival in an anaplastic thyroid cancer model.
Cytochrome c release is upstream to activation of caspase-9, caspase-8, and caspase-3 in the enhanced apoptosis of anaplastic thyroid cancer cells induced by manumycin and paclitaxel.
Modulation of parathyroid hormone-related protein levels (PTHrP) in anaplastic thyroid cancer.
p21 Waf-1 (Cip-1) enhances apoptosis induced by manumycin and paclitaxel in anaplastic thyroid cancer cells.
Redox Control of Manumycin A-Induced Apoptosis in Anaplastic Thyroid Cancer Cells: Involvement of the Xenobiotic Apoptotic Pathway.
Triple Negative Breast Neoplasms
Low-Dose Farnesyltransferase Inhibitor Suppresses HIF-1? and Snail Expression in Triple-Negative Breast Cancer MDA-MB-231 Cells In Vitro.
Uterine Cervical Neoplasms
Correlation between high salt intake and mortality rates for oesophageal and gastric cancers in Henan Province, China.
Vascular Diseases
Farnesyltransferase inhibitor R115777 protects against vascular disease in uremic mice.
Vitreoretinopathy, Proliferative
Role of inhibitors of isoprenylation in proliferation, phenotype and apoptosis of human retinal pigment epithelium.