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Disease on EC 2.5.1.10 - (2E,6E)-farnesyl diphosphate synthase

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DISEASE
TITLE OF PUBLICATION
LINK TO PUBMED
Alzheimer Disease
Multistage screening reveals chameleon ligands of the human farnesyl pyrophosphate synthase: implications to drug discovery for neurodegenerative diseases.
Atherosclerosis
Inhibition of farnesyl pyrophosphate synthase attenuates high glucose?induced vascular smooth muscle cells proliferation.
Bone Diseases
3D-QSAR, molecular docking, and ONIOM studies on the structure-activity relationships and action mechanism of nitrogen-containing bisphosphonates.
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery.
Discovery of Novel Allosteric Non-Bisphosphonate Inhibitors of Farnesyl Pyrophosphate Synthase by Integrated Lead Finding.
Fragment-Based Discovery of Non-bisphosphonate Binders of Trypanosoma brucei Farnesyl Pyrophosphate Synthase.
Key Enzymes for the Mevalonate Pathway in the Cardiovascular System.
Mono- and dialkyl isoprenoid bisphosphonates as geranylgeranyl diphosphate synthase inhibitors.
Pharmacophore Mapping of Thienopyrimidine-Based Monophosphonate (ThP-MP) Inhibitors of the Human Farnesyl Pyrophosphate Synthase.
Structural Basis for the Exceptional in vivo Efficacy of Bisphosphonate Drugs.
Thienopyrimidine Bisphosphonate (ThPBP) Inhibitors of the Human Farnesyl Pyrophosphate Synthase: Optimization and Characterization of the Mode of Inhibition.
Zoledronate repositioning as a potential trypanocidal drug. Trypanosoma cruzi HPRT an alternative target to be considered.
Bone Diseases, Metabolic
Correlation between time-dependent inhibition of human farnesyl pyrophosphate synthase and blockade of mevalonate pathway by nitrogen-containing bisphosphonates in cultured cells.
Bone Resorption
A novel inhibitory mechanism of nitrogen-containing bisphosphonate on the activity of Cl- extrusion in osteoclasts.
An investigation of bone resorption and Dictyostelium discoideum growth inhibition by bisphosphonate drugs.
Bisphosphonates are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase.
Bisphosphonates: Future perspective for neurological disorders.
Differentiating the mechanisms of antiresorptive action of nitrogen containing bisphosphonates.
Drug insight: Bisphosphonates for postmenopausal osteoporosis.
Engineered gene over-expression as a method of drug target identification.
Farnesyl diphosphate synthase inhibitors from in silico screening.
Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries.
Farnesyl Pyrophosphate Synthase as a Target for Drug Development: Discovery of Natural-Product-Derived Inhibitors and Their Activity in Pancreatic Cancer Cells.
Identification of a bisphosphonate that inhibits isopentenyl diphosphate isomerase and farnesyl diphosphate synthase.
Identification of a novel phosphonocarboxylate inhibitor of Rab geranylgeranyl transferase that specifically prevents Rab prenylation in osteoclasts and macrophages.
In Vitro and In Vivo Responses to High and Low Doses of Nitrogen-Containing Bisphosphonates Suggest Engagement of Different Mechanisms for Inhibition of Osteoclastic Bone Resorption.
Inhibition of protein prenylation by bisphosphonates causes sustained activation of Rac, Cdc42, and Rho GTPases.
Isoprenoid biosynthesis as a drug target: bisphosphonate inhibition of Escherichia coli K12 growth and synergistic effects of fosmidomycin.
Minodronate for the treatment of osteoporosis.
Mono- and dialkyl isoprenoid bisphosphonates as geranylgeranyl diphosphate synthase inhibitors.
Pyridinium-1-yl bisphosphonates are potent inhibitors of farnesyl diphosphate synthase and bone resorption.
Selective in vitro effects of the farnesyl pyrophosphate synthase inhibitor risedronate on Trypanosoma cruzi.
Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates.
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
The inhibition of human farnesyl pyrophosphate synthase by nitrogen-containing bisphosphonates. Elucidating the role of active site threonine 201 and tyrosine 204 residues using enzyme mutants.
Thienopyrimidine Bisphosphonate (ThPBP) Inhibitors of the Human Farnesyl Pyrophosphate Synthase: Optimization and Characterization of the Mode of Inhibition.
[Muscle and bone health as a risk factor of fall among the elderly. Prevention of fracture and bisphosphonate]
[Pharmacokinetics of Zoledronic acid[once-yearly bisphosphonate(intravenous infusion)].]
Brain Neoplasms
Deregulated expression and activity of Farnesyl Diphosphate Synthase (FDPS) in Glioblastoma.
The isoprenoid derivative N(6) -benzyladenosine CM223 exerts antitumor effects in glioma patient-derived primary cells through the mevalonate pathway.
Breast Neoplasms
Pamidronate resistance and associated low ras levels in breast cancer cells: a role for combinatorial therapy.
Carcinoma, Hepatocellular
Hepatic farnesyl diphosphate synthase expression is suppressed by polyunsaturated fatty acids.
Isolation and sequence of the human farnesyl pyrophosphate synthetase cDNA. Coordinate regulation of the mRNAs for farnesyl pyrophosphate synthetase, 3-hydroxy-3-methylglutaryl coenzyme A reductase, and 3-hydroxy-3-methylglutaryl coenzyme A synthase by phorbol ester.
Cardiomegaly
Alteration of RhoA Prenylation Ameliorates Cardiac and Vascular Remodeling in Spontaneously Hypertensive Rats.
Cardiac-specific overexpression of farnesyl pyrophosphate synthase induces cardiac hypertrophy and dysfunction in mice.
Chronic inhibition of farnesyl pyrophosphate synthase attenuates cardiac hypertrophy and fibrosis in spontaneously hypertensive rats.
Inhibition of farnesyl pyrophosphate synthase attenuates angiotensin II-induced cardiac hypertrophy and fibrosis in vivo.
Cardiovascular Diseases
Establishment of transgenic mice carrying the gene for farnesyl pyrophosphate synthase
Establishment of transgenic mice carrying the gene for farnesyl pyrophosphate synthase.
Key Enzymes for the Mevalonate Pathway in the Cardiovascular System.
Lentiviral-Mediated Silencing of Farnesyl Pyrophosphate Synthase through RNA Interference in Mice.
Chagas Disease
1-(Fluoroalkylidene)-1,1-bisphosphonic acids are potent and selective inhibitors of the enzymatic activity of Toxoplasma gondii farnesyl pyrophosphate synthase.
Antiparasitic Activity of Sulfur- and Fluorine-Containing Bisphosphonates against Trypanosomatids and Apicomplexan Parasites.
Computational Drug Repositioning by Target Hopping: A Use Case in Chagas Disease.
Establishing Trypanosoma cruzi farnesyl pyrophosphate synthase as a viable target for biosensor driven fragment-based lead discovery.
New insights into molecular recognition of 1,1-bisphosphonic acids by farnesyl diphosphate synthase.
Synthesis and biological evaluation of 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase.
Synthesis and biological evaluation of new 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase.
Colorectal Neoplasms
A significant role of lipogenic enzymes in colorectal cancer.
Higher farnesyl diphosphate synthase activity in human colorectal cancer inhibition of cellular apoptosis.
Communicable Diseases
Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries.
Deficiency Diseases
Farnesyl-diphosphate synthase is localized in peroxisomes.
Diabetic Cardiomyopathies
Expression of farnesyl pyrophosphate synthase is increased in diabetic cardiomyopathy.
Enzootic Bovine Leukosis
Oncoviral bovine leukemia virus G4 and human T-cell leukemia virus type 1 p13(II) accessory proteins interact with farnesyl pyrophosphate synthetase.
Glioblastoma
Deregulated expression and activity of Farnesyl Diphosphate Synthase (FDPS) in Glioblastoma.
Farnesyl diphosphate synthase attenuates paclitaxel-induced apoptotic cell death in human glioblastoma U87MG cells.
Farnesyl diphosphate synthase is important for the maintenance of glioblastoma stemness.
p53 regulates the mevalonate pathway in human glioblastoma multiforme.
Heart Failure
Key Enzymes for the Mevalonate Pathway in the Cardiovascular System.
Hepatitis C
Viperin: a radical response to viral infection.
Hepatoblastoma
Sterol-regulatory-element-binding protein 2 and nuclear factor Y control human farnesyl diphosphate synthase expression and affect cell proliferation in hepatoblastoma cells.
Hypercholesterolemia
Lead nitrate-induced development of hypercholesterolemia in rats: sterol-independent gene regulation of hepatic enzymes responsible for cholesterol homeostasis.
Hyperlipidemias
Key Enzymes for the Mevalonate Pathway in the Cardiovascular System.
Hypertension
Establishment of transgenic mice carrying the gene for farnesyl pyrophosphate synthase
Establishment of transgenic mice carrying the gene for farnesyl pyrophosphate synthase.
Inhibition of farnesyl pyrophosphate synthase prevents norepinephrine-induced fibrotic responses in vascular smooth muscle cells from spontaneously hypertensive rats.
Hypertrophy, Left Ventricular
Chronic inhibition of farnesyl pyrophosphate synthase attenuates cardiac hypertrophy and fibrosis in spontaneously hypertensive rats.
Influenza, Human
Investigating the efficacy of pamidronate, a chemical inhibitor of farnesyl pyrophosphate synthase, in the inhibition of influenza virus infection in vitro and in vivo.
Receptor tyrosine kinase inhibitors block multiple steps of influenza a virus replication.
Leukemia
Isolation and sequence of the human farnesyl pyrophosphate synthetase cDNA. Coordinate regulation of the mRNAs for farnesyl pyrophosphate synthetase, 3-hydroxy-3-methylglutaryl coenzyme A reductase, and 3-hydroxy-3-methylglutaryl coenzyme A synthase by phorbol ester.
Leukemia, Lymphoid
Geranylgeranyl diphosphate synthase inhibition induces apoptosis that is dependent upon GGPP depletion, ERK phosphorylation and caspase activation.
Leukemia, T-Cell
Oncoviral bovine leukemia virus G4 and human T-cell leukemia virus type 1 p13(II) accessory proteins interact with farnesyl pyrophosphate synthetase.
Leukemia-Lymphoma, Adult T-Cell
Human T-Lymphotropic Virus Type 1 Mitochondrion-Localizing Protein p13II Is Required for Viral Infectivity In Vivo.
Malaria
Chemo-Immunotherapeutic Anti-Malarials Targeting Isoprenoid Biosynthesis.
Specific Inhibition of the Bifunctional Farnesyl/Geranylgeranyl Diphosphate Synthase in Malaria Parasites via a New Small-Molecule Binding Site.
Multiple Myeloma
Design and Synthesis of Active Site Inhibitors of the Human Farnesyl Pyrophosphate Synthase - Apoptosis and Inhibition of ERK Phosphorylation in Multiple Myeloma Cells.
Pharmacogenetics of bisphosphonate-associated osteonecrosis of the jaw.
Neoplasm Metastasis
Cancer metastasis therapeutic targets and drug discovery: emerging small-molecule protein kinase inhibitors.
Thienopyrimidine Bisphosphonate (ThPBP) Inhibitors of the Human Farnesyl Pyrophosphate Synthase: Optimization and Characterization of the Mode of Inhibition.
Neoplasms
Biochemical changes of mevalonate pathway in human colorectal cancer.
Bisphosphonate-induced ATP analog formation and its effect on inhibition of cancer cell growth.
Bisphosphonates: preclinical review.
Cancer metastasis therapeutic targets and drug discovery: emerging small-molecule protein kinase inhibitors.
Comparison of ?? T cell responses and farnesyl diphosphate synthase inhibition in tumor cells pretreated with zoledronic acid.
Current Advances in ?? T Cell-Based Tumor Immunotherapy.
Design of potent bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase via targeted interactions with the active site 'capping' phenyls.
Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries.
Farnesyl Pyrophosphate Synthase as a Target for Drug Development: Discovery of Natural-Product-Derived Inhibitors and Their Activity in Pancreatic Cancer Cells.
FDPS cooperates with PTEN loss to promote prostate cancer progression through modulation of small GTPases/AKT axis.
FPPS mediates TGF-?1-induced non-small cell lung cancer cell invasion and the EMT process via the RhoA/Rock1 pathway.
In vivo phosphoantigen levels in bisphosphonate-treated human breast tumors trigger V?9V?2 T-cell antitumor cytotoxicity through ICAM-1 engagement.
Inhibitors of prenyl transferases.
Mevalonate pathway intermediates downregulate zoledronic acid- induced isopentenyl pyrophosphate and ATP analog formation in human breast cancer cells.
N6-isopentenyladenosine arrests tumor cell proliferation by inhibiting farnesyl diphosphate synthase and protein prenylation.
Nano-technology based carriers for nitrogen-containing bisphosphonates delivery as sensitisers of ?? T cells for anticancer immunotherapy.
Nonpeptide antigens, presentation mechanisms, and immunological memory of human Vgamma2Vdelta2 T cells: discriminating friend from foe through the recognition of prenyl pyrophosphate antigens.
Reduced expression of the mevalonate pathway enzyme farnesyl pyrophosphate synthase unveils recognition of tumor cells by Vgamma9Vdelta2 T cells.
Self-assembling nanoparticles encapsulating zoledronic acid revert multidrug resistance in cancer cells.
The bisphosphonate zoledronic acid has antimyeloma activity in vivo by inhibition of protein prenylation.
The crystal structure of human geranylgeranyl pyrophosphate synthase reveals a novel hexameric arrangement and inhibitory product binding.
Thienopyrimidine Bisphosphonate (ThPBP) Inhibitors of the Human Farnesyl Pyrophosphate Synthase: Optimization and Characterization of the Mode of Inhibition.
Various pathways of zoledronic acid against osteoclasts and bone cancer metastasis: a brief review.
Neuroblastoma
24S-hydroxycholesterol effects on lipid metabolism genes are modeled in traumatic brain injury.
Neurodegenerative Diseases
Multistage screening reveals chameleon ligands of the human farnesyl pyrophosphate synthase: implications to drug discovery for neurodegenerative diseases.
Osteolysis
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery.
Osteoporosis
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery.
Association of farnesyl diphosphate synthase polymorphisms and response to alendronate treatment in Chinese postmenopausal women with osteoporosis.
Bisphosphonates: Future perspective for neurological disorders.
Key Enzymes for the Mevalonate Pathway in the Cardiovascular System.
Mono- and dialkyl isoprenoid bisphosphonates as geranylgeranyl diphosphate synthase inhibitors.
Protonation State and Hydration of Bisphosphonate Bound to Farnesyl Pyrophosphate Synthase.
Synergistic action of statins and nitrogen-containing bisphosphonates in the development of rhabdomyolysis in L6 rat skeletal myoblasts.
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
The crystal structure of human geranylgeranyl pyrophosphate synthase reveals a novel hexameric arrangement and inhibitory product binding.
Thienopyrimidine Bisphosphonate (ThPBP) Inhibitors of the Human Farnesyl Pyrophosphate Synthase: Optimization and Characterization of the Mode of Inhibition.
Osteoporosis, Postmenopausal
Modulatory effect of farnesyl pyrophosphate synthase (FDPS) rs2297480 polymorphism on the response to long-term amino-bisphosphonate treatment in postmenopausal osteoporosis.
Osteosarcoma
Farnesyl diphosphate synthase is involved in the resistance to zoledronic acid of osteosarcoma cells.
Ovarian Neoplasms
Inhibition of the mevalonate pathway augments the activity of pitavastatin against ovarian cancer cells.
Pancreatic Neoplasms
Farnesyl Pyrophosphate Synthase as a Target for Drug Development: Discovery of Natural-Product-Derived Inhibitors and Their Activity in Pancreatic Cancer Cells.
Parasitic Diseases
New insights into molecular recognition of 1,1-bisphosphonic acids by farnesyl diphosphate synthase.
Porokeratosis
Disorder of the mevalonate pathway inhibits calcium-induced differentiation of keratinocytes.
Prostatic Neoplasms
Altered expression of farnesyl pyrophosphate synthase in prostate cancer: evidence for a role of the mevalonate pathway in disease progression?
FDPS cooperates with PTEN loss to promote prostate cancer progression through modulation of small GTPases/AKT axis.
Pharmacogenetics of bisphosphonate-associated osteonecrosis of the jaw.
Schistosomiasis
Characterization of farnesyl diphosphate synthase and geranylgeranyl diphosphate synthase in Schistosoma mansoni: potential drug targets.
Stomach Neoplasms
Insights into the mevalonate pathway in the anticancer effect of a platinum complex on human gastric cancer cells.
Toxoplasmosis
1-(Fluoroalkylidene)-1,1-bisphosphonic acids are potent and selective inhibitors of the enzymatic activity of Toxoplasma gondii farnesyl pyrophosphate synthase.
Antiparasitic Activity of Sulfur- and Fluorine-Containing Bisphosphonates against Trypanosomatids and Apicomplexan Parasites.
New insights into molecular recognition of 1,1-bisphosphonic acids by farnesyl diphosphate synthase.
Trypanosomiasis, African
Crystallization and preliminary X-ray diffraction study of the farnesyl diphosphate synthase from Trypanosoma brucei.
In Vitro and In Vivo Investigation of the Inhibition of Trypanosoma brucei Cell Growth by Lipophilic Bisphosphonates.
Tuberculosis
Identification of a novel class of omega,E,E-farnesyl diphosphate synthase from Mycobacterium tuberculosis.
Virus Diseases
Investigating the efficacy of pamidronate, a chemical inhibitor of farnesyl pyrophosphate synthase, in the inhibition of influenza virus infection in vitro and in vivo.