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Literature summary for 2.5.1.10 extracted from

  • 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 (2019), J. Med. Chem., 62, 10867-10896 .
    View publication on PubMed
Search for more literature for 2.5.1.10

Inhibitors

Inhibitors Comment Organism Structure
(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
(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
(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
(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
(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
(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
(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
(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
11,12-dihydroxy-7,20-epoxyabieta-8,11,13-trien-20-one
-
 Homo sapiens
11,12-dihydroxy-N-(2-hydroxyethyl)abieta-8(14),9(11),12-trien-20-amide
-
 Homo sapiens
11,12-dihydroxy-N-methylabieta-8(14),9(11),12-trien-20-amide
-
 Homo sapiens
11,12-dihydroxy-N-[(pyridin-3-yl)methyl]abieta-8(14),9(11),12-trien-20-amide
-
 Homo sapiens
11,12-dihydroxy-N-[3-(1H-imidazol-1-yl)propyl]abieta-8(14),9(11),12-trien-20-amide
-
 Homo sapiens
11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide
-
 Homo sapiens
12-hydroxy-11,20-epoxyabieta-8(14),9(11),12-trien-20-one
-
 Homo sapiens
2-[11,12-dihydroxy-20-oxoabieta-8(14),9(11),12-trien-20-yl]hydrazine-1-carboxamide
-
 Homo sapiens
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
6,20-epoxyabieta-8,13-diene-7,11,12,20-tetrone
-
 Homo sapiens
7,20-epoxyabieta-8(14),9(11),12-triene-11,12-diol
-
 Homo sapiens
7,20-epoxyabieta-8,13-diene-11,12,20-trione
-
 Homo sapiens
7,20-epoxyabieta-8,13-diene-11,12-dione
-
 Homo sapiens
abieta-8(14),9(11),12-triene-11,12,20-triol
-
 Homo sapiens
methyl 11,12-dihydroxy-7-(phenylsulfanyl)abieta-8(14),9(11),12-trien-20-oate
-
 Homo sapiens
methyl 11,12-dihydroxy-7-methoxyabieta-8(14),9(11),12-trien-20-oate
-
 Homo sapiens
methyl 11,12-dihydroxy-7-oxoabieta-8(14),9(11),12-trien-20-oate
-
 Homo sapiens
methyl 11,12-dihydroxy-7-[(2-hydroxyethyl)sulfanyl]abieta-8(14),9(11),12-trien-20-oate
-
 Homo sapiens
methyl 11,12-dihydroxyabieta-7,9(11),13-trien-20-oate
-
 Homo sapiens
methyl 11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate
-
 Homo sapiens
methyl 11-[[tert-butyl(dimethyl)silyl]oxy]-12-hydroxyabieta-8(14),9(11),12-trien-20-oate
-
 Homo sapiens
methyl 7,11,12-trioxoabieta-8,13-dien-20-oate
-
 Homo sapiens
methyl 7-(butylsulfanyl)-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate
-
 Homo sapiens
methyl 7-ethoxy-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate
-
 Homo sapiens
methyl 7-ethoxy-11,12-dioxoabieta-8,13-dien-20-oate
-
 Homo sapiens
methyl 7-tert-butoxy-11,12-dioxoabieta-8,13-dien-20-oate
-
 Homo sapiens
methyl 7-[(2-hydroxyethyl)sulfanyl]-11,12-dioxoabieta-8,13-dien-20-oate
-
 Homo sapiens
N'-(4-bromobenzoyl)-11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide
-
 Homo sapiens
N'-acetyl-11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide
-
 Homo sapiens
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
N-benzyl-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-amide
-
 Homo sapiens
N-[2-(dimethylamino)ethyl]-11,12-dihydroxy-7-oxoabieta-8(14),9(11),12-trien-20-amide
-
 Homo sapiens
N-[2-(dimethylamino)ethyl]-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-amide
-
 Homo sapiens
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
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
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
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
zoledronate
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
dimethylallyl diphosphate + isopentenyl diphosphate Homo sapiens reaction of EC 2.5.1.1, the enzyme catalyzes the condensation of dimethylallyl pyrophosphate and isopentenyl pyrophosphate, forming geranyl pyrophosphate and then farnesyl pyrophosphate diphosphate + geranyl diphosphate
-
 ?
geranyl diphosphate + isopentenyl diphosphate Homo sapiens the enzyme catalyzes the condensation of dimethylallyl pyrophosphate and isopentenyl pyrophosphate, forming geranyl pyrophosphate and then farnesyl pyrophosphate diphosphate + (2E,6E)-farnesyl diphosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P14324
-
-

Source Tissue

Source Tissue Comment Organism Textmining
pancreatic cancer cell line
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
dimethylallyl diphosphate + isopentenyl diphosphate reaction of EC 2.5.1.1, the enzyme catalyzes the condensation of dimethylallyl pyrophosphate and isopentenyl pyrophosphate, forming geranyl pyrophosphate and then farnesyl pyrophosphate Homo sapiens diphosphate + geranyl diphosphate
-
 ?
geranyl diphosphate + isopentenyl diphosphate the enzyme catalyzes the condensation of dimethylallyl pyrophosphate and isopentenyl pyrophosphate, forming geranyl pyrophosphate and then farnesyl pyrophosphate Homo sapiens diphosphate + (2E,6E)-farnesyl diphosphate
-
 ?

Synonyms

Synonyms Comment Organism
farnesyl pyrophosphate synthase
-
 Homo sapiens
FPPS
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
23
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0001
-
 pH 7.5, 23°C Homo sapiens zoledronate
0.000194
-
 pH 7.5, 23°C Homo sapiens (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
0.000234
-
 pH 7.5, 23°C Homo sapiens methyl 7-tert-butoxy-11,12-dioxoabieta-8,13-dien-20-oate
0.000252
-
 pH 7.5, 23°C Homo sapiens 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
0.000289
-
 pH 7.5, 23°C Homo sapiens (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
0.000335
-
 pH 7.5, 23°C Homo sapiens (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
0.000389
-
 pH 7.5, 23°C Homo sapiens 6,20-epoxyabieta-8,13-diene-7,11,12,20-tetrone
0.000473
-
 pH 7.5, 23°C Homo sapiens 7,20-epoxyabieta-8,13-diene-11,12,20-trione
0.00052
-
 pH 7.5, 23°C Homo sapiens tert-butyl [(1R)-1-amino-2-[2-[11,12-dihydroxy-20-oxoabieta-8(14),9(11),12-trien-20-yl]hydrazinyl]-2-oxoethyl]carbamate
0.000523
-
 pH 7.5, 23°C Homo sapiens methyl 7,11,12-trioxoabieta-8,13-dien-20-oate
0.000596
-
 pH 7.5, 23°C Homo sapiens 7,20-epoxyabieta-8,13-diene-11,12-dione
0.000644
-
 pH 7.5, 23°C Homo sapiens 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
0.0008
-
 pH 7.5, 23°C Homo sapiens N'-(4-bromobenzoyl)-11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide
0.000833
-
 pH 7.5, 23°C Homo sapiens methyl 11,12-dihydroxyabieta-7,9(11),13-trien-20-oate
0.000859
-
 pH 7.5, 23°C Homo sapiens (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
0.000865
-
 pH 7.5, 23°C Homo sapiens methyl 11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate
0.000914
-
 pH 7.5, 23°C Homo sapiens 11,12-dihydroxy-N-(2-hydroxyethyl)abieta-8(14),9(11),12-trien-20-amide
0.0011
-
 pH 7.5, 23°C Homo sapiens (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
0.0011
-
 pH 7.5, 23°C Homo sapiens methyl 11,12-dihydroxy-7-methoxyabieta-8(14),9(11),12-trien-20-oate
0.0012
-
 pH 7.5, 23°C Homo sapiens N-[2-(dimethylamino)ethyl]-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-amide
0.0013
-
 pH 7.5, 23°C Homo sapiens methyl 11,12-dihydroxy-7-[(2-hydroxyethyl)sulfanyl]abieta-8(14),9(11),12-trien-20-oate
0.0015
-
 pH 7.5, 23°C Homo sapiens N'-acetyl-11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide
0.0022
-
 pH 7.5, 23°C Homo sapiens (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
0.0027
-
 pH 7.5, 23°C Homo sapiens 11,12-dihydroxy-N-methylabieta-8(14),9(11),12-trien-20-amide
0.0027
-
 pH 7.5, 23°C Homo sapiens 11,12-dihydroxy-N-[(pyridin-3-yl)methyl]abieta-8(14),9(11),12-trien-20-amide
0.0031
-
 pH 7.5, 23°C Homo sapiens 2-[11,12-dihydroxy-20-oxoabieta-8(14),9(11),12-trien-20-yl]hydrazine-1-carboxamide
0.00603
-
 pH 7.5, 23°C Homo sapiens N-benzyl-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-amide
0.0074
-
 pH 7.5, 23°C Homo sapiens 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
0.0078
-
 pH 7.5, 23°C Homo sapiens abieta-8(14),9(11),12-triene-11,12,20-triol
0.008
-
 pH 7.5, 23°C Homo sapiens 11,12-dihydroxy-N-[3-(1H-imidazol-1-yl)propyl]abieta-8(14),9(11),12-trien-20-amide
0.008
-
 pH 7.5, 23°C Homo sapiens N-[2-(dimethylamino)ethyl]-11,12-dihydroxy-7-oxoabieta-8(14),9(11),12-trien-20-amide
0.0086
-
 pH 7.5, 23°C Homo sapiens methyl 7-ethoxy-11,12-dioxoabieta-8,13-dien-20-oate
0.0106
-
 pH 7.5, 23°C Homo sapiens 12-hydroxy-11,20-epoxyabieta-8(14),9(11),12-trien-20-one
0.0125
-
 pH 7.5, 23°C Homo sapiens methyl 7-(butylsulfanyl)-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate
0.0125
-
 pH 7.5, 23°C Homo sapiens 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
0.0133
-
 pH 7.5, 23°C Homo sapiens 11,12-dihydroxy-7,20-epoxyabieta-8,11,13-trien-20-one
0.0133
-
 pH 7.5, 23°C Homo sapiens methyl 7-ethoxy-11,12-dihydroxyabieta-8(14),9(11),12-trien-20-oate
0.0137
-
 pH 7.5, 23°C Homo sapiens (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
0.0187
-
 pH 7.5, 23°C Homo sapiens 7,20-epoxyabieta-8(14),9(11),12-triene-11,12-diol
0.0227
-
 pH 7.5, 23°C Homo sapiens methyl 7-[(2-hydroxyethyl)sulfanyl]-11,12-dioxoabieta-8,13-dien-20-oate
0.0251
-
 pH 7.5, 23°C Homo sapiens (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
0.02564
-
 pH 7.5, 23°C Homo sapiens 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
0.028
-
 pH 7.5, 23°C Homo sapiens methyl 11,12-dihydroxy-7-(phenylsulfanyl)abieta-8(14),9(11),12-trien-20-oate
0.035
-
 pH 7.5, 23°C Homo sapiens 11,12-dihydroxyabieta-8(14),9(11),12-triene-20-hydrazide
0.0412
-
 pH 7.5, 23°C Homo sapiens methyl 11,12-dihydroxy-7-oxoabieta-8(14),9(11),12-trien-20-oate
0.0563
-
 pH 7.5, 23°C Homo sapiens methyl 11-[[tert-butyl(dimethyl)silyl]oxy]-12-hydroxyabieta-8(14),9(11),12-trien-20-oate

General Information

General Information Comment Organism
drug target the enzyme is a target for treating bone resorption diseases and some cancers Homo sapiens