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(((2-phenylthieno[2,3-d]pyrimidin-4-yl)amino)methylene)diphosphonic acid
-
about 75% inhibition at 0.01 mM
(((5-phenylthieno[2,3-d]pyrimidin-4-yl)amino)methylene)diphosphonic acid
-
about 10% inhibition at 0.01 mM
(((6-(4-tolyl)thieno[2,3-d]pyrimidin-4-yl)amino)methylene)diphosphonic acid
-
about 85% inhibition at 0.01 mM
(((6-(naphthalen-2-yl)thieno[2,3-d]pyrimidin-4-yl)amino)methylene)diphosphonic acid
-
about 87% inhibition at 0.01 mM
(4bR,8aS)-4b-(5-acetyl-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-5,6,7,8,8a,9-hexahydrophenanthrene-3,4,10(4bH)-trione
-
(4bR,8aS)-4b-(5-amino-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol
-
(4bR,8aS)-4b-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol
-
(4bR,8aS)-4b-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-5,6,7,8,8a,9-hexahydrophenanthrene-3,4,10(4bH)-trione
-
(4bR,8aS)-4b-(5-[(1S)-1-[(hydroxymethyl)amino]ethyl]-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol
-
(4bR,8aS)-4b-[5-(4-bromophenyl)-1,3,4-oxadiazol-2-yl]-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol
-
(4bR,8aS)-4b-[5-(4-bromophenyl)-1,3,4-oxadiazol-2-yl]-8,8-dimethyl-2-(propan-2-yl)-5,6,7,8,8a,9-hexahydrophenanthrene-3,4,10(4bH)-trione
-
(4bR,8aS)-4b-[5-[(dimethylamino)methyl]-1,3,4-oxadiazol-2-yl]-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol
-
(6-phenylthieno[2,3-d]pyrimidin-4-ylamino)methylenebisphosphonic acid
-
about 61% inhibition at 0.01 mM
(R)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-(3-fluorophenyl)ethyl)phosphonic acid
-
(R)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-cyclohexylethyl)phosphonic acid
-
(R)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-phenylethyl)phosphonic acid
-
(R)-(2-(3-fluorophenyl)-1-((6-(p-tolyl)thieno[2,3-d]-pyrimidin-4-yl)amino)ethyl)phosphonic acid
-
(R)-(2-phenyl-1-((6-(p-tolyl)thieno[2,3-d]pyrimidin-4-yl)-amino)ethyl)phosphonic acid
-
(R)-2-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-3-(3-fluorophenyl)propanoic acid
-
(S)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-(3-fluorophenyl)ethyl)phosphonic acid
-
(S)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-cyclohexylethyl)phosphonic acid
-
(S)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-phenylethyl)phosphonic acid
-
(S)-(2-(3-fluorophenyl)-1-((6-(p-tolyl)thieno[2,3-d]-pyrimidin-4-yl)amino)ethyl)phosphonic acid
-
(S)-(2-phenyl-1-((6-(p-tolyl)thieno[2,3-d]pyrimidin-4-yl)-amino)ethyl)phosphonic acid
-
(thieno[2,3-d]pyrimidin-4-ylamino)methylene bisphosphonic acid
-
about 78% inhibition at 0.01 mM
([[6-(1-methyl-1H-pyrazol-4-yl)pyridin-3-yl]amino]methanediyl)bis(phosphonic acid)
-
([[6-(3-methoxyphenyl)pyridin-3-yl]amino]methanediyl)bis(phosphonic acid)
-
([[6-(4-methylphenyl)-5,6-dihydrothieno[2,3-d]pyrimidin-4-yl]amino]methyl)phosphonic acid
-
([[6-(thiophen-3-yl)pyridin-3-yl]amino]methanediyl)bis(phosphonic acid)
-
1-(carboxymethyl)-1H-benzo[g]indole-2-carboxylic acid
-
1-(carboxymethyl)-5,9b-dihydro-1H-benzo[g]indole-2-carboxylic acid
-
1-[(3-carboxy-1,2-oxazol-5-yl)methyl]-1H-benzo[g]indole-2-carboxylic acid
-
-
1-[(benzyloxy)carbonyl]-2,3-dihydro-1H-indole-2-carboxylic acid
-
-
11,12-dihydroxy-7,20-epoxyabieta-8,11,13-trien-20-one
-
11,12-dihydroxy-N-(2-hydroxyethyl)abieta-8(14),9(11),12-trien-20-amide
-
11,12-dihydroxy-N-methylabieta-8(14),9(11),12-trien-20-amide
-
11,12-dihydroxy-N-[(pyridin-3-yl)methyl]abieta-8(14),9(11),12-trien-20-amide
-
11,12-dihydroxy-N-[3-(1H-imidazol-1-yl)propyl]abieta-8(14),9(11),12-trien-20-amide
-
11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide
-
11-hydroxyabieta-7,9(11),13-triene-6,12-dione
-
12-hydroxy-11,20-epoxyabieta-8(14),9(11),12-trien-20-one
-
1H,1'H-4,4'-biindole-2-carboxylic acid
-
-
2,6,7-trihydroxy-9-(2-hydroxyphenyl)-4,4a-dihydro-3H-xanthen-3-one
-
2-(naphthalen-1-ylmethoxy)-4-(phenylamino)benzoic acid
-
-
2-(naphthalen-1-ylmethoxy)benzoic acid
-
-
2-[11,12-dihydroxy-20-oxoabieta-8(14),9(11),12-trien-20-yl]hydrazine-1-carboxamide
-
2-[[(1S,2R,4aR)-4a-hydroxy-1,2-dimethyl-5-methylidenedecahydronaphthalen-1-yl]methyl]cyclohexa-2,5-diene-1,4-dione
-
3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
-
-
4'-(hydroxymethyl)-3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
-
-
4'-(methylcarbamoyl)-3-[(naphthalen-1-yl)methoxy][1,1'-biphenyl]-4-carboxylic acid
-
-
4'-acetamido-3-[(naphthalen-1-yl)methoxy][1,1'-biphenyl]-4-carboxylic acid
-
-
4'-carbamoyl-3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
-
-
4'-fluoro-3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
-
-
4'-[(methanesulfonyl)amino]-3-[(naphthalen-1-yl)methoxy][1,1'-biphenyl]-4-carboxylic acid
-
-
4-(1,3-benzodioxol-5-yl)-2-(naphthalen-1-ylmethoxy)benzoic acid
-
-
4-(1-methyl-1H-indol-5-yl)-2-[(naphthalen-1-yl)methoxy]benzoic acid
-
-
4-(1H-indol-5-yl)-2-(naphthalen-1-ylmethoxy)benzoic acid
-
-
4-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-[(naphthalen-1-yl)methoxy]benzoic acid
-
-
4-(6-methoxynaphthalen-2-yl)-2-[(naphthalen-1-yl)methoxy]benzoic acid
-
-
4-(naphthalen-1-yl)-1H-indole-2-carboxylic acid
-
-
4-[5-[(4aR,10aS)-5,6-dihydroxy-1,1-dimethyl-7-(propan-2-yl)-1,3,4,9,10,10a-hexahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]benzonitrile
-
6,20-epoxyabieta-8,13-diene-7,11,12,20-tetrone
-
6-amino-5-ethoxy-8-(naphthalen-1-yl)quinoline-2-carboxylic acid
-
-
6-amino-8-(naphthalen-1-yl)quinoline-2-carboxylic acid
-
-
6-[(ethoxycarbonyl)amino]-8-(naphthalen-1-yl)quinoline-2-carboxylic acid
-
-
7,20-epoxyabieta-8(14),9(11),12-triene-11,12-diol
-
7,20-epoxyabieta-8,13-diene-11,12,20-trione
-
7,20-epoxyabieta-8,13-diene-11,12-dione
-
8-(1H-indol-4-yl)quinoline-2-carboxylic acid
-
-
8-(naphthalen-1-yl)-6-(1H-pyrrol-2-yl)quinoline-2-carboxylic acid
-
-
8-(naphthalen-1-yl)-6-(thiophen-3-yl)quinoline-2-carboxylic acid
-
-
8-(naphthalen-1-yl)quinoline-2-carboxylic acid
-
-
abieta-8(14),9(11),12-triene-11,12,20-triol
-
farnesyl diphosphate
allosteric product inhibition. the product can trap the enzyme in an unreactive state by binding to its allosteric pocket
isopentenyl diphosphate
-
-
methyl 11,12-dihydroxy-7-(phenylsulfanyl)abieta-8(14),9(11),12-trien-20-oate
-
methyl 11,12-dihydroxy-7-methoxyabieta-8(14),9(11),12-trien-20-oate
-
methyl 11,12-dihydroxy-7-oxoabieta-8(14),9(11),12-trien-20-oate
-
methyl 11,12-dihydroxy-7-[(2-hydroxyethyl)sulfanyl]abieta-8(14),9(11),12-trien-20-oate
-
methyl 11,12-dihydroxyabieta-7,9(11),13-trien-20-oate
-
methyl 11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate
-
methyl 11-[[tert-butyl(dimethyl)silyl]oxy]-12-hydroxyabieta-8(14),9(11),12-trien-20-oate
-
methyl 7,11,12-trioxoabieta-8,13-dien-20-oate
-
methyl 7-(butylsulfanyl)-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate
-
methyl 7-ethoxy-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate
-
methyl 7-ethoxy-11,12-dioxoabieta-8,13-dien-20-oate
-
methyl 7-tert-butoxy-11,12-dioxoabieta-8,13-dien-20-oate
-
methyl 7-[(2-hydroxyethyl)sulfanyl]-11,12-dioxoabieta-8,13-dien-20-oate
-
N'-(4-bromobenzoyl)-11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide
-
N'-acetyl-11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide
-
N-acetyl-S-((4aR,10aS)-5,6-dihydroxy-7-isopropyl-4a-(methoxycarbonyl)-1,1-dimethyl-1,2,3,4,4a,9,10,10a-octahydrophenanthren-9-yl)-L-cysteine
-
N-benzyl-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-amide
-
N-[2-(dimethylamino)ethyl]-11,12-dihydroxy-7-oxoabieta-8(14),9(11),12-trien-20-amide
-
N-[2-(dimethylamino)ethyl]-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-amide
-
tert-butyl [(1R)-1-amino-2-[2-[11,12-dihydroxy-20-oxoabieta-8(14),9(11),12-trien-20-yl]hydrazinyl]-2-oxoethyl]carbamate
-
tert-butyl [(1R)-1-[5-[(4aR,10aS)-5,6-dihydroxy-1,1-dimethyl-9-oxo-7-(propan-2-yl)-1,3,4,9,10,10a-hexahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]ethyl]carbamate
-
tert-butyl [(1S)-1-[5-[(4aR,10aS)-1,1-dimethyl-5,6,9-trioxo-7-(propan-2-yl)-1,3,4,5,6,9,10,10a-octahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]ethyl]carbamate
-
tert-butyl [(1S)-1-[5-[(4aR,10aS)-5,6-dihydroxy-1,1-dimethyl-7-(propan-2-yl)-1,3,4,9,10,10a-hexahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]ethyl]carbamate
-
ZINC04011866
0.01 mM, 29.9% inhibition
ZINC04043066
0.01 mM, 25.3% inhibition
ZINC04064228
0.01 mM, 11.5% inhibition
ZINC04082083
0.01 mM, 17.3% inhibition
ZINC04763743
0.01 mM, 29.4% inhibition
ZINC05037497
0.01 mM, 29.3% inhibition
ZINC06894343
0.01 mM, 28.9% inhibition
ZINC09224949
0.01 mM, 23.5% inhibition
ZINC12377242
0.01 mM, 13% inhibition
ZINC15868804
0.01 mM, 24% inhibition
[([6-[3-(trifluoromethyl)phenyl]pyridin-3-yl]amino)methanediyl]bis(phosphonic acid)
-
[({4-[4-(propan-2-yloxy)phenyl]pyridin-2-yl}amino)methanediyl]bis(phosphonic acid)
-
about 90% inhibition at 0.01 mM
[1-fluoro-2-[2-(1H-indazol-4-yl)pyridin-4-yl]ethane-1,1-diyl]bis(phosphonic acid)
-
[1-fluoro-2-[5-(1H-indazol-4-yl)pyridin-2-yl]ethane-1,1-diyl]bis(phosphonic acid)
-
[1-fluoro-2-[5-(1H-indazol-4-yl)pyridin-3-yl]ethane-1,1-diyl]bis(phosphonic acid)
-
[1-fluoro-2-[5-(1H-indazol-5-yl)pyridin-2-yl]ethane-1,1-diyl]bis(phosphonic acid)
-
[1-fluoro-2-[5-(1H-indazol-5-yl)pyridin-3-yl]ethane-1,1-diyl]bis(phosphonic acid)
-
[1-fluoro-2-[5-(1H-indazol-6-yl)pyridin-3-yl]ethane-1,1-diyl]bis(phosphonic acid)
-
[1-fluoro-2-[5-(1H-pyrazol-4-yl)pyridin-2-yl]ethane-1,1-diyl]bis(phosphonic acid)
-
[1-fluoro-2-[5-(1H-pyrazol-4-yl)pyridin-3-yl]ethane-1,1-diyl]bis(phosphonic acid)
-
[1-fluoro-2-[6-(1H-pyrazol-4-yl)pyridin-3-yl]ethane-1,1-diyl]bis(phosphonic acid)
-
[2-(1,2-dimethyl-1H-indol-3-yl)ethane-1,1-diyl]bis(phosphonic acid)
about 64% inhibition at 0.01 mM
[2-(1-ethyl-1H-indol-3-yl)ethane-1,1-diyl]bis(phosphonic acid)
about 78% inhibition at 0.01 mM
[2-(1-methyl-1H-indol-3-yl)ethane-1,1-diyl]bis(phosphonic acid)
about 60% inhibition at 0.01 mM
[2-(2-methyl-1H-indol-3-yl)ethane-1,1-diyl]bis(phosphonic acid)
about 30% inhibition at 0.01 mM
[2-(2-tert-butyl-1H-indol-3-yl)ethane-1,1-diyl]bis(phosphonic acid)
about 79% inhibition at 0.01 mM
[2-[2-(3,5-dimethyl-1,2-oxazol-4-yl)pyridin-4-yl]-1-fluoroethane-1,1-diyl]bis(phosphonic acid)
-
[2-[5-(3,5-dimethyl-1,2-oxazol-4-yl)pyridin-3-yl]-1-fluoroethane-1,1-diyl]bis(phosphonic acid)
-
[2-[6-(3,5-dimethyl-1,2-oxazol-4-yl)pyridin-2-yl]-1-fluoroethane-1,1-diyl]bis(phosphonic acid)
-
[6,7-dihydro-5H-cyclopenta[c]pyridin-7-yl(hydroxy)methylene]bis(phosphonic acid)
i.e. NE-10501, chiral analog of risedronate. Crystallization of human enzyme from a solution of racemic NE-10501 results in a complex containing the R enantiomer in the enzyme active site
{2-[(1-methyl-1H-imidazo[4,5-b]pyridin-2-yl)amino]ethane-1,1-diyl}bis(phosphonic acid)
about 65% inhibition at 0.01 mM
{2-[(3-methyl-3H-imidazo[4,5-b]pyridin-2-yl)amino]ethane-1,1-diyl}bis(phosphonic acid)
about 10% inhibition at 0.01 mM
{2-[1-(propan-2-yl)-1H-indol-3-yl]ethane-1,1-diyl}bis(phosphonic acid)
about 45% inhibition at 0.01 mM
{2-[2-(1-cyclopentylethyl)-1H-indol-3-yl]ethane-1,1-diyl}bis(phosphonic acid)
about 90% inhibition at 0.01 mM
{2-[2-(3-methylbutan-2-yl)-1H-indol-3-yl]ethane-1,1-diyl}bis(phosphonic acid)
about 85% inhibition at 0.01 mM
{2-[2-(3-methylbutan-2-yl)-5-phenyl-1H-indol-3-yl]ethane-1,1-diyl}bis(phosphonic acid)
about 95% inhibition at 0.01 mM
alendronate
-
pamidronate
-
risedronate
about 98% inhibition at 100 mM
zoledronate
-
zoledronic acid
-
-
additional information
Monte carlo optimization method using CORAL software is used successfully for designing a statistically robust QSAR model for human farnesyl pyrophosphate synthase inhibitors
-
additional information
-
Monte carlo optimization method using CORAL software is used successfully for designing a statistically robust QSAR model for human farnesyl pyrophosphate synthase inhibitors
-
additional information
the enzyme possesses three inhibition binding sites: the allylic site (dimethyl allyl pyrophosphate and geranyl pyrophosphate), the homoallylic site (isopentenyl pyrophosphate), and the allosteric site. Bisphosphonate-based inhibitors are extremely effective inhibitors binding to the allylic site
-
additional information
-
the enzyme possesses three inhibition binding sites: the allylic site (dimethyl allyl pyrophosphate and geranyl pyrophosphate), the homoallylic site (isopentenyl pyrophosphate), and the allosteric site. Bisphosphonate-based inhibitors are extremely effective inhibitors binding to the allylic site
-
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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.
Bone Diseases
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery.
Bone Diseases
Discovery of Novel Allosteric Non-Bisphosphonate Inhibitors of Farnesyl Pyrophosphate Synthase by Integrated Lead Finding.
Bone Diseases
Fragment-Based Discovery of Non-bisphosphonate Binders of Trypanosoma brucei Farnesyl Pyrophosphate Synthase.
Bone Diseases
Key Enzymes for the Mevalonate Pathway in the Cardiovascular System.
Bone Diseases
Mono- and dialkyl isoprenoid bisphosphonates as geranylgeranyl diphosphate synthase inhibitors.
Bone Diseases
Pharmacophore Mapping of Thienopyrimidine-Based Monophosphonate (ThP-MP) Inhibitors of the Human Farnesyl Pyrophosphate Synthase.
Bone Diseases
Structural Basis for the Exceptional in vivo Efficacy of Bisphosphonate Drugs.
Bone Diseases
Thienopyrimidine Bisphosphonate (ThPBP) Inhibitors of the Human Farnesyl Pyrophosphate Synthase: Optimization and Characterization of the Mode of Inhibition.
Bone Diseases
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.
Bone Resorption
An investigation of bone resorption and Dictyostelium discoideum growth inhibition by bisphosphonate drugs.
Bone Resorption
Bisphosphonates are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase.
Bone Resorption
Bisphosphonates: Future perspective for neurological disorders.
Bone Resorption
Differentiating the mechanisms of antiresorptive action of nitrogen containing bisphosphonates.
Bone Resorption
Drug insight: Bisphosphonates for postmenopausal osteoporosis.
Bone Resorption
Engineered gene over-expression as a method of drug target identification.
Bone Resorption
Farnesyl diphosphate synthase inhibitors from in silico screening.
Bone Resorption
Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries.
Bone Resorption
Farnesyl Pyrophosphate Synthase as a Target for Drug Development: Discovery of Natural-Product-Derived Inhibitors and Their Activity in Pancreatic Cancer Cells.
Bone Resorption
Identification of a bisphosphonate that inhibits isopentenyl diphosphate isomerase and farnesyl diphosphate synthase.
Bone Resorption
Identification of a novel phosphonocarboxylate inhibitor of Rab geranylgeranyl transferase that specifically prevents Rab prenylation in osteoclasts and macrophages.
Bone Resorption
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.
Bone Resorption
Inhibition of protein prenylation by bisphosphonates causes sustained activation of Rac, Cdc42, and Rho GTPases.
Bone Resorption
Isoprenoid biosynthesis as a drug target: bisphosphonate inhibition of Escherichia coli K12 growth and synergistic effects of fosmidomycin.
Bone Resorption
Minodronate for the treatment of osteoporosis.
Bone Resorption
Mono- and dialkyl isoprenoid bisphosphonates as geranylgeranyl diphosphate synthase inhibitors.
Bone Resorption
Pyridinium-1-yl bisphosphonates are potent inhibitors of farnesyl diphosphate synthase and bone resorption.
Bone Resorption
Selective in vitro effects of the farnesyl pyrophosphate synthase inhibitor risedronate on Trypanosoma cruzi.
Bone Resorption
Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates.
Bone Resorption
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.
Bone Resorption
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.
Bone Resorption
Thienopyrimidine Bisphosphonate (ThPBP) Inhibitors of the Human Farnesyl Pyrophosphate Synthase: Optimization and Characterization of the Mode of Inhibition.
Bone Resorption
[Muscle and bone health as a risk factor of fall among the elderly. Prevention of fracture and bisphosphonate]
Bone Resorption
[Pharmacokinetics of Zoledronic acid[once-yearly bisphosphonate(intravenous infusion)].]
Brain Neoplasms
Deregulated expression and activity of Farnesyl Diphosphate Synthase (FDPS) in Glioblastoma.
Brain Neoplasms
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.
Carcinoma, Hepatocellular
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.
Cardiomegaly
Cardiac-specific overexpression of farnesyl pyrophosphate synthase induces cardiac hypertrophy and dysfunction in mice.
Cardiomegaly
Chronic inhibition of farnesyl pyrophosphate synthase attenuates cardiac hypertrophy and fibrosis in spontaneously hypertensive rats.
Cardiomegaly
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
Cardiovascular Diseases
Establishment of transgenic mice carrying the gene for farnesyl pyrophosphate synthase.
Cardiovascular Diseases
Key Enzymes for the Mevalonate Pathway in the Cardiovascular System.
Cardiovascular Diseases
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.
Chagas Disease
Antiparasitic Activity of Sulfur- and Fluorine-Containing Bisphosphonates against Trypanosomatids and Apicomplexan Parasites.
Chagas Disease
Computational Drug Repositioning by Target Hopping: A Use Case in Chagas Disease.
Chagas Disease
Establishing Trypanosoma cruzi farnesyl pyrophosphate synthase as a viable target for biosensor driven fragment-based lead discovery.
Chagas Disease
New insights into molecular recognition of 1,1-bisphosphonic acids by farnesyl diphosphate synthase.
Chagas Disease
Synthesis and biological evaluation of 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase.
Chagas Disease
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.
Colorectal Neoplasms
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.
Glioblastoma
Farnesyl diphosphate synthase attenuates paclitaxel-induced apoptotic cell death in human glioblastoma U87MG cells.
Glioblastoma
Farnesyl diphosphate synthase is important for the maintenance of glioblastoma stemness.
Glioblastoma
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
Hypertension
Establishment of transgenic mice carrying the gene for farnesyl pyrophosphate synthase.
Hypertension
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.
Influenza, Human
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.
Malaria
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.
Multiple Myeloma
Pharmacogenetics of bisphosphonate-associated osteonecrosis of the jaw.
Neoplasm Metastasis
Cancer metastasis therapeutic targets and drug discovery: emerging small-molecule protein kinase inhibitors.
Neoplasm Metastasis
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.
Neoplasms
Bisphosphonate-induced ATP analog formation and its effect on inhibition of cancer cell growth.
Neoplasms
Bisphosphonates: preclinical review.
Neoplasms
Cancer metastasis therapeutic targets and drug discovery: emerging small-molecule protein kinase inhibitors.
Neoplasms
Comparison of ?? T cell responses and farnesyl diphosphate synthase inhibition in tumor cells pretreated with zoledronic acid.
Neoplasms
Current Advances in ?? T Cell-Based Tumor Immunotherapy.
Neoplasms
Design of potent bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase via targeted interactions with the active site 'capping' phenyls.
Neoplasms
Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries.
Neoplasms
Farnesyl Pyrophosphate Synthase as a Target for Drug Development: Discovery of Natural-Product-Derived Inhibitors and Their Activity in Pancreatic Cancer Cells.
Neoplasms
FDPS cooperates with PTEN loss to promote prostate cancer progression through modulation of small GTPases/AKT axis.
Neoplasms
FPPS mediates TGF-?1-induced non-small cell lung cancer cell invasion and the EMT process via the RhoA/Rock1 pathway.
Neoplasms
In vivo phosphoantigen levels in bisphosphonate-treated human breast tumors trigger V?9V?2 T-cell antitumor cytotoxicity through ICAM-1 engagement.
Neoplasms
Inhibitors of prenyl transferases.
Neoplasms
Mevalonate pathway intermediates downregulate zoledronic acid- induced isopentenyl pyrophosphate and ATP analog formation in human breast cancer cells.
Neoplasms
N6-isopentenyladenosine arrests tumor cell proliferation by inhibiting farnesyl diphosphate synthase and protein prenylation.
Neoplasms
Nano-technology based carriers for nitrogen-containing bisphosphonates delivery as sensitisers of ?? T cells for anticancer immunotherapy.
Neoplasms
Nonpeptide antigens, presentation mechanisms, and immunological memory of human Vgamma2Vdelta2 T cells: discriminating friend from foe through the recognition of prenyl pyrophosphate antigens.
Neoplasms
Reduced expression of the mevalonate pathway enzyme farnesyl pyrophosphate synthase unveils recognition of tumor cells by Vgamma9Vdelta2 T cells.
Neoplasms
Self-assembling nanoparticles encapsulating zoledronic acid revert multidrug resistance in cancer cells.
Neoplasms
The bisphosphonate zoledronic acid has antimyeloma activity in vivo by inhibition of protein prenylation.
Neoplasms
The crystal structure of human geranylgeranyl pyrophosphate synthase reveals a novel hexameric arrangement and inhibitory product binding.
Neoplasms
Thienopyrimidine Bisphosphonate (ThPBP) Inhibitors of the Human Farnesyl Pyrophosphate Synthase: Optimization and Characterization of the Mode of Inhibition.
Neoplasms
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.
Osteoporosis
Association of farnesyl diphosphate synthase polymorphisms and response to alendronate treatment in Chinese postmenopausal women with osteoporosis.
Osteoporosis
Bisphosphonates: Future perspective for neurological disorders.
Osteoporosis
Key Enzymes for the Mevalonate Pathway in the Cardiovascular System.
Osteoporosis
Mono- and dialkyl isoprenoid bisphosphonates as geranylgeranyl diphosphate synthase inhibitors.
Osteoporosis
Protonation State and Hydration of Bisphosphonate Bound to Farnesyl Pyrophosphate Synthase.
Osteoporosis
Synergistic action of statins and nitrogen-containing bisphosphonates in the development of rhabdomyolysis in L6 rat skeletal myoblasts.
Osteoporosis
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.
Osteoporosis
The crystal structure of human geranylgeranyl pyrophosphate synthase reveals a novel hexameric arrangement and inhibitory product binding.
Osteoporosis
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?
Prostatic Neoplasms
FDPS cooperates with PTEN loss to promote prostate cancer progression through modulation of small GTPases/AKT axis.
Prostatic Neoplasms
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.
Toxoplasmosis
Antiparasitic Activity of Sulfur- and Fluorine-Containing Bisphosphonates against Trypanosomatids and Apicomplexan Parasites.
Toxoplasmosis
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.
Trypanosomiasis, African
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.
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0.000289
(4bR,8aS)-4b-(5-acetyl-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-5,6,7,8,8a,9-hexahydrophenanthrene-3,4,10(4bH)-trione
Homo sapiens
pH 7.5, 23°C
0.000859
(4bR,8aS)-4b-(5-amino-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol
Homo sapiens
pH 7.5, 23°C
0.0022
(4bR,8aS)-4b-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol
Homo sapiens
pH 7.5, 23°C
0.000335
(4bR,8aS)-4b-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-5,6,7,8,8a,9-hexahydrophenanthrene-3,4,10(4bH)-trione
Homo sapiens
pH 7.5, 23°C
0.000194
(4bR,8aS)-4b-(5-[(1S)-1-[(hydroxymethyl)amino]ethyl]-1,3,4-oxadiazol-2-yl)-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol
Homo sapiens
pH 7.5, 23°C
0.0251
(4bR,8aS)-4b-[5-(4-bromophenyl)-1,3,4-oxadiazol-2-yl]-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol
Homo sapiens
pH 7.5, 23°C
0.0137
(4bR,8aS)-4b-[5-(4-bromophenyl)-1,3,4-oxadiazol-2-yl]-8,8-dimethyl-2-(propan-2-yl)-5,6,7,8,8a,9-hexahydrophenanthrene-3,4,10(4bH)-trione
Homo sapiens
pH 7.5, 23°C
0.0011
(4bR,8aS)-4b-[5-[(dimethylamino)methyl]-1,3,4-oxadiazol-2-yl]-8,8-dimethyl-2-(propan-2-yl)-4b,5,6,7,8,8a,9,10-octahydrophenanthrene-3,4-diol
Homo sapiens
pH 7.5, 23°C
0.081
1-(carboxymethyl)-1H-benzo[g]indole-2-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.0133
11,12-dihydroxy-7,20-epoxyabieta-8,11,13-trien-20-one
Homo sapiens
pH 7.5, 23°C
0.000914
11,12-dihydroxy-N-(2-hydroxyethyl)abieta-8(14),9(11),12-trien-20-amide
Homo sapiens
pH 7.5, 23°C
0.0027
11,12-dihydroxy-N-methylabieta-8(14),9(11),12-trien-20-amide
Homo sapiens
pH 7.5, 23°C
0.0027
11,12-dihydroxy-N-[(pyridin-3-yl)methyl]abieta-8(14),9(11),12-trien-20-amide
Homo sapiens
pH 7.5, 23°C
0.008
11,12-dihydroxy-N-[3-(1H-imidazol-1-yl)propyl]abieta-8(14),9(11),12-trien-20-amide
Homo sapiens
pH 7.5, 23°C
0.035
11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide
Homo sapiens
pH 7.5, 23°C
0.0012 - 0.0024
11-hydroxyabieta-7,9(11),13-triene-6,12-dione
0.0106
12-hydroxy-11,20-epoxyabieta-8(14),9(11),12-trien-20-one
Homo sapiens
pH 7.5, 23°C
0.0139
1H,1'H-4,4'-biindole-2-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.081
2,6,7-trihydroxy-9-(2-hydroxyphenyl)-4,4a-dihydro-3H-xanthen-3-one
Homo sapiens
pH and temperature not specified in the publication
0.02
2-(naphthalen-1-ylmethoxy)-4-(phenylamino)benzoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0068
2-(naphthalen-1-ylmethoxy)benzoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0031
2-[11,12-dihydroxy-20-oxoabieta-8(14),9(11),12-trien-20-yl]hydrazine-1-carboxamide
Homo sapiens
pH 7.5, 23°C
0.0011
2-[[(1S,2R,4aR)-4a-hydroxy-1,2-dimethyl-5-methylidenedecahydronaphthalen-1-yl]methyl]cyclohexa-2,5-diene-1,4-dione
Homo sapiens
pH and temperature not specified in the publication
0.00085
3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000058
4'-(hydroxymethyl)-3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00014
4'-(methylcarbamoyl)-3-[(naphthalen-1-yl)methoxy][1,1'-biphenyl]-4-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000017
4'-acetamido-3-[(naphthalen-1-yl)methoxy][1,1'-biphenyl]-4-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00011
4'-carbamoyl-3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00008
4'-fluoro-3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00123
4'-[(methanesulfonyl)amino]-3-[(naphthalen-1-yl)methoxy][1,1'-biphenyl]-4-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000049
4-(1,3-benzodioxol-5-yl)-2-(naphthalen-1-ylmethoxy)benzoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00027
4-(1-methyl-1H-indol-5-yl)-2-[(naphthalen-1-yl)methoxy]benzoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00019
4-(1H-indol-5-yl)-2-(naphthalen-1-ylmethoxy)benzoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00025
4-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-[(naphthalen-1-yl)methoxy]benzoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000038
4-(6-methoxynaphthalen-2-yl)-2-[(naphthalen-1-yl)methoxy]benzoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0071
4-(naphthalen-1-yl)-1H-indole-2-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0074
4-[5-[(4aR,10aS)-5,6-dihydroxy-1,1-dimethyl-7-(propan-2-yl)-1,3,4,9,10,10a-hexahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]benzonitrile
Homo sapiens
pH 7.5, 23°C
0.000389
6,20-epoxyabieta-8,13-diene-7,11,12,20-tetrone
Homo sapiens
pH 7.5, 23°C
0.000024
6-amino-5-ethoxy-8-(naphthalen-1-yl)quinoline-2-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000069
6-amino-8-(naphthalen-1-yl)quinoline-2-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000037
6-[(ethoxycarbonyl)amino]-8-(naphthalen-1-yl)quinoline-2-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0187
7,20-epoxyabieta-8(14),9(11),12-triene-11,12-diol
Homo sapiens
pH 7.5, 23°C
0.000473
7,20-epoxyabieta-8,13-diene-11,12,20-trione
Homo sapiens
pH 7.5, 23°C
0.000596
7,20-epoxyabieta-8,13-diene-11,12-dione
Homo sapiens
pH 7.5, 23°C
0.02
8-(1H-indol-4-yl)quinoline-2-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000077
8-(naphthalen-1-yl)-6-(1H-pyrrol-2-yl)quinoline-2-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
8-(naphthalen-1-yl)-6-(thiophen-3-yl)quinoline-2-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0012
8-(naphthalen-1-yl)quinoline-2-carboxylic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0078
abieta-8(14),9(11),12-triene-11,12,20-triol
Homo sapiens
pH 7.5, 23°C
0.0011
arenarone
Homo sapiens
pH and temperature not specified in the publication
0.2
celastrol
Homo sapiens
IC50 above 0.2 mM, pH and temperature not specified in the publication
0.028
methyl 11,12-dihydroxy-7-(phenylsulfanyl)abieta-8(14),9(11),12-trien-20-oate
Homo sapiens
pH 7.5, 23°C
0.0011
methyl 11,12-dihydroxy-7-methoxyabieta-8(14),9(11),12-trien-20-oate
Homo sapiens
pH 7.5, 23°C
0.0412
methyl 11,12-dihydroxy-7-oxoabieta-8(14),9(11),12-trien-20-oate
Homo sapiens
pH 7.5, 23°C
0.0013
methyl 11,12-dihydroxy-7-[(2-hydroxyethyl)sulfanyl]abieta-8(14),9(11),12-trien-20-oate
Homo sapiens
pH 7.5, 23°C
0.000833
methyl 11,12-dihydroxyabieta-7,9(11),13-trien-20-oate
Homo sapiens
pH 7.5, 23°C
0.000865
methyl 11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate
Homo sapiens
pH 7.5, 23°C
0.0563
methyl 11-[[tert-butyl(dimethyl)silyl]oxy]-12-hydroxyabieta-8(14),9(11),12-trien-20-oate
Homo sapiens
pH 7.5, 23°C
0.000523
methyl 7,11,12-trioxoabieta-8,13-dien-20-oate
Homo sapiens
pH 7.5, 23°C
0.0125
methyl 7-(butylsulfanyl)-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate
Homo sapiens
pH 7.5, 23°C
0.0133
methyl 7-ethoxy-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate
Homo sapiens
pH 7.5, 23°C
0.0086
methyl 7-ethoxy-11,12-dioxoabieta-8,13-dien-20-oate
Homo sapiens
pH 7.5, 23°C
0.000234
methyl 7-tert-butoxy-11,12-dioxoabieta-8,13-dien-20-oate
Homo sapiens
pH 7.5, 23°C
0.0227
methyl 7-[(2-hydroxyethyl)sulfanyl]-11,12-dioxoabieta-8,13-dien-20-oate
Homo sapiens
pH 7.5, 23°C
0.0008
N'-(4-bromobenzoyl)-11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide
Homo sapiens
pH 7.5, 23°C
0.0015
N'-acetyl-11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide
Homo sapiens
pH 7.5, 23°C
0.02564
N-acetyl-S-((4aR,10aS)-5,6-dihydroxy-7-isopropyl-4a-(methoxycarbonyl)-1,1-dimethyl-1,2,3,4,4a,9,10,10a-octahydrophenanthren-9-yl)-L-cysteine
Homo sapiens
pH 7.5, 23°C
0.00603
N-benzyl-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-amide
Homo sapiens
pH 7.5, 23°C
0.008
N-[2-(dimethylamino)ethyl]-11,12-dihydroxy-7-oxoabieta-8(14),9(11),12-trien-20-amide
Homo sapiens
pH 7.5, 23°C
0.0012
N-[2-(dimethylamino)ethyl]-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-amide
Homo sapiens
pH 7.5, 23°C
0.0012
taxodione
Homo sapiens
pH and temperature not specified in the publication
0.0024
taxodone
Homo sapiens
pH and temperature not specified in the publication
0.00052
tert-butyl [(1R)-1-amino-2-[2-[11,12-dihydroxy-20-oxoabieta-8(14),9(11),12-trien-20-yl]hydrazinyl]-2-oxoethyl]carbamate
Homo sapiens
pH 7.5, 23°C
0.0125
tert-butyl [(1R)-1-[5-[(4aR,10aS)-5,6-dihydroxy-1,1-dimethyl-9-oxo-7-(propan-2-yl)-1,3,4,9,10,10a-hexahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]ethyl]carbamate
Homo sapiens
pH 7.5, 23°C
0.000252
tert-butyl [(1S)-1-[5-[(4aR,10aS)-1,1-dimethyl-5,6,9-trioxo-7-(propan-2-yl)-1,3,4,5,6,9,10,10a-octahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]ethyl]carbamate
Homo sapiens
pH 7.5, 23°C
0.000644
tert-butyl [(1S)-1-[5-[(4aR,10aS)-5,6-dihydroxy-1,1-dimethyl-7-(propan-2-yl)-1,3,4,9,10,10a-hexahydrophenanthren-4a(2H)-yl]-1,3,4-oxadiazol-2-yl]ethyl]carbamate
Homo sapiens
pH 7.5, 23°C
0.0001
zoledronate
Homo sapiens
pH 7.5, 23°C
0.0006295
[6,7-dihydro-5H-cyclopenta[c]pyridin-7-yl(hydroxy)methylene]bis(phosphonic acid)
Homo sapiens
racemat
0.0012
11-hydroxyabieta-7,9(11),13-triene-6,12-dione
Homo sapiens
pH and temperature not specified in the publication
0.0024
11-hydroxyabieta-7,9(11),13-triene-6,12-dione
Homo sapiens
pH and temperature not specified in the publication
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Barnard, G.F.
Prenyltransferase from human liver
Methods Enzymol.
110
155-171
1985
Homo sapiens
brenda
Deprele, S.; Kashemirov, B.A.; Hogan,J.M.; Ebetino, F.H.; Barnett, B.L.; Evdokimov, A.; McKenna, C.E.
Farnesyl pyrophosphate synthase enantiospecificity with a chiral risedronate analog, [6,7-dihydro-5H-cyclopenta[c]pyridin-7-yl(hydroxy)methylene]bis(phosphonic acid) (NE-10501): Synthetic, structural, and modeling studies
Bioorg. Med. Chem. Lett.
18
2878-2882
2008
Homo sapiens (P14324), Homo sapiens
brenda
Li, J.; Herold, M.J.; Kimmel, B.; Mueller, I.; Rincon-Orozco, B.; Kunzmann, V.; Herrmann, T.
Reduced expression of the mevalonate pathway enzyme farnesyl pyrophosphate synthase unveils recognition of tumor cells by Vgamma9Vdelta2 T cells
J. Immunol.
182
8118-8124
2009
Homo sapiens
brenda
De Schutter, J.; Zaretsky, S.; Welbourn, S.; Pause, A.; Tsantrizos, Y.
Novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase
Bioorg. Med. Chem. Lett.
20
5781-5786
2010
Homo sapiens (P14324), Homo sapiens
brenda
Das, S.; Edwards, P.A.; Crockett, J.C.; Rogers, M.J.
Upregulation of endogenous farnesyl diphosphate synthase overcomes the inhibitory effect of bisphosphonate on protein prenylation in Hela cells
Biochim. Biophys. Acta
1841
569-573
2014
Homo sapiens
brenda
Gritzalis, D.; Park, J.; Chiu, W.; Cho, H.; Lin, Y.S.; De Schutter, J.W.; Lacbay, C.M.; Zielinski, M.; Berghuis, A.M.; Tsantrizos, Y.S.
Probing the molecular and structural elements of ligands binding to the active site versus an allosteric pocket of the human farnesyl pyrophosphate synthase
Bioorg. Med. Chem. Lett.
25
1117-1123
2015
Homo sapiens (P14324), Homo sapiens
brenda
Leung, C.Y.; Langille, A.M.; Mancuso, J.; Tsantrizos, Y.S.
Discovery of thienopyrimidine-based inhibitors of the human farnesyl pyrophosphate synthase - parallel synthesis of analogs via a trimethylsilyl ylidene intermediate
Bioorg. Med. Chem.
21
2229-2240
2013
Homo sapiens
brenda
Marzinzik, A.L.; Amstutz, R.; Bold, G.; Bourgier, E.; Cotesta, S.; Glickman, J.F.; Goette, M.; Henry, C.; Lehmann, S.; Hartwieg, J.C.; Ofner, S.; Pelle, X.; Roddy, T.P.; Rondeau, J.M.; Stauffer, F.; Stout, S.J.; Widmer, A.; Zimmermann, J.; Zoller, T.; Jahnke, W.
Discovery of novel allosteric non-bisphosphonate inhibitors of farnesyl pyrophosphate synthase by integrated lead finding
ChemMedChem
10
1884-1891
2015
Homo sapiens
brenda
Liu, Y.L.; Lindert, S.; Zhu, W.; Wang, K.; McCammon, J.A.; Oldfield, E.
Taxodione and arenarone inhibit farnesyl diphosphate synthase by binding to the isopentenyl diphosphate site
Proc. Natl. Acad. Sci. USA
111
E2530-E2539
2014
Trypanosoma brucei, Homo sapiens (P14324), Homo sapiens
brenda
Kumar, P.; Kumar, A.; Sindhu, J.; Lal, S.
QSAR models for nitrogen containing monophosphonate and bisphosphonate derivatives as human farnesyl pyrophosphate synthase inhibitors based on Monte Carlo method
Drug Res.
69
159-167
2019
Homo sapiens (P14324), Homo sapiens
brenda
Liu, Q.; Miao, Y.; Wang, X.; Lv, G.; Peng, Y.; Li, K.; Li, M.; Qiu, L.; Lin, J.
Structure-based virtual screening and biological evaluation of novel non-bisphosphonate farnesyl pyrophosphate synthase inhibitors
Eur. J. Med. Chem.
186
111905
2020
Homo sapiens (P14324)
brenda
Rodriguez, J.B.; Falcone, B.N.; Szajnman, S.H.
Approaches for designing new potent inhibitors of farnesyl pyrophosphate synthase
Expert Opin. Drug Discov.
11
307-320
2016
Homo sapiens (P14324), Homo sapiens
brenda
Fernandez, D.; Ramis, R.; Ortega-Castro, J.; Casasnovas, R.; Vilanova, B.; Frau, J.
New insights into human farnesyl pyrophosphate synthase inhibition by second-generation bisphosphonate drugs
J. Comput. Aided Mol. Des.
31
675-688
2017
Homo sapiens (P14324), Homo sapiens
brenda
Han, S.; Li, X.; Xia, Y.; Yu, Z.; Cai, N.; Malwal, S.R.; Han, X.; Oldfield, E.; Zhang, Y.
Farnesyl pyrophosphate synthase as a target for drug development discovery of natural-product-derived inhibitors and their activity in pancreatic cancer cells
J. Med. Chem.
62
10867-10896
2019
Homo sapiens (P14324), Homo sapiens
brenda
Feng, Y.; Park, J.; Li, S.G.; Boutin, R.; Viereck, P.; Schilling, M.A.; Berghuis, A.M.; Tsantrizos, Y.S.
Chirality-driven mode of binding of alpha-aminophosphonic acid-based allosteric inhibitors of the human farnesyl pyrophosphate synthase (hFPPS)
J. Med. Chem.
62
9691-9702
2019
Homo sapiens (P14324), Homo sapiens
brenda
Park, J.; Zielinski, M.; Magder, A.; Tsantrizos, Y.S.; Berghuis, A.M.
Human farnesyl pyrophosphate synthase is allosterically inhibited by its own product
Nat. Commun.
8
14132
2017
Homo sapiens (P14324), Homo sapiens
brenda
Park, J.; Rodionov, D.; De Schutter, J.W.; Lin, Y.S.; Tsantrizos, Y.S.; Berghuis, A.M.
Crystallographic and thermodynamic characterization of phenylaminopyridine bisphosphonates binding to human farnesyl pyrophosphate synthase
PLoS ONE
12
e0186447
2017
Homo sapiens (P14324), Homo sapiens
brenda