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Farnesyl-Diphosphate Farnesyltransferase

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Definition: The first committed enzyme of the biosynthesis pathway that leads to the production of STEROLS. it catalyzes the synthesis of SQUALENE from farnesyl pyrophosphate via the intermediate PRESQUALENE PYROPHOSPHATE. This enzyme is also a critical branch point enzyme in the biosynthesis of ISOPRENOIDS that is thought to regulate the flux of isoprene intermediates through the sterol pathway.      Other names Squalene Synthetase; Transferase, FPP-FPP Farnesyl; Synthetase, Squalene; Synthase, Squalene; Synthase, Presqualene-Diphosphate; Presqualene Diphosphate Synthase; Farnesyltransferase, Farnesyldiphosphate-Farnesyld; Farnesyltransferase, Farnesyl-Diphosphate; Farnesyldiphosphate Farnesyldiphosphate Farnesyltr; Farnesyl Transferase, FPP-FPP; Farnesyl Diphosphate Farnesyltransferase; FPP FPP Farnesyl Transferase; Squalene Synthase; Presqualene-Diphosphate Synthase; Farnesyldiphosphate-Farnesyldiphosphate Farnesyltr; FPP-FPP Farnesyl Transferase
 
SubstanceCAS Registry & nameCategoriesSourceDrugs*
1-(4-((4-chloro-2-((2-chlorophenyl)(hydroxy)methyl)phenyl)(2,2-dimethylpropyl)amino)-4-oxobutanoyl)piperidine-3-carboxylic acid  0   *Benzhydryl Compounds *Piperidines Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. Bioorg Med Chem 2011 Mar 15;19(6):1930-49
ERG9 protein, S cerevisiae  EC 2.5.1.21   *Farnesyl-Diphosphate Farnesyltransferase *Saccharomyces cerevisiae Proteins.
3-((2-benzyl-6-(3-methoxypropyloxy)pyridin-3-yl)ethynyl)quinuclidin-3-ol  0   *Pyridines *Quinuclidines Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. Antimicrob Agents Chemother 2004 Jul;48(7):2379-87
3-((2-benzyl-6-(3-hydroxy-4-methoxypyrrolidin-1-yl)pyridin-3-yl)ethynyl)quinuclidin-3-ol  0   *Pyridines *Quinuclidines Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. Antimicrob Agents Chemother 2004 Jul;48(7):2379-87
1-((1-(3-acetoxy-2,2-dimethylpropyl)-7-chloro-5-(2,3-dimethoxyphenyl)-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepin-3-yl)acetyl)piperidine-4-acetic acid  0   *Oxazepines *Piperidines Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. J Med Chem 2002 Sep 26;45(20):4571-80
phomoidride C  0   *Maleic Anhydrides Farnesyl-Diphosphate Farnesyltransferase. Org Lett 2001 May 17;3(10):1443-5
phomoidride D  0   *Maleic Anhydrides Farnesyl-Diphosphate Farnesyltransferase. Org Lett 2001 May 17;3(10):1443-5
YM 53601  0   *Quinuclidines Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. Br J Pharmacol 2000 Sep;131(1):63-70
ER 27856  0   *Diphosphonates Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. J Lipid Res 2000 Jul;41(7):1136-44
ER 28448  0   *Diphosphonates Farnesyl-Diphosphate Farnesyltransferase. J Lipid Res 2000 Jul;41(7):1136-44
zaragozic acid D3  0   *Tricarboxylic Acids *Bicyclo Compounds, Heterocyclic Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. J Antibiot (Tokyo) 1998 Apr;51(4):428-31
F 10863B  0   *Dicarboxylic Acids *Bicyclo Compounds, Heterocyclic Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. J Antibiot (Tokyo) 1998 Apr;51(4):428-31
BMS 187745  0   *Sulfonic Acids Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. Toxicol Appl Pharmacol 1997 Jul;145(1):91-8
A 87049  0   *Amides *Dicarboxylic Acids Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. J Med Chem 1997 Jul 4;40(14):2123-5
viridiofungin C  0   *Citrates Tryptophan/*analogs & derivatives Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. J Antibiot (Tokyo) 1997 Apr;50(4):339-43
viridiofungin B  0   *Citrates Phenylalanine/*analogs & derivatives Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. J Antibiot (Tokyo) 1997 Apr;50(4):339-43
viridiofungin A  0   *Citrates Tyrosine/*analogs & derivatives Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. J Antibiot (Tokyo) 1997 Apr;50(4):339-43
CP 225917  0   *Maleic Anhydrides Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. J Antibiot (Tokyo) 1997 Jan;50(1):1-7
BMS 188494-04  0   *Sulfonic Acids Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. J Chromatogr A 1996 Jul 19;739(1-2):343-9; Toxicol Appl Pharmacol 1997 Jul;145(1):91-8
schizostatin  0   *Fatty Acids *Fumarates Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. J Antibiot (Tokyo) 1996 Jul;49(7):617-23
3-(4-(pyrid-4-yl)phenyl)-3-hydroxyquinuclidine  0   *Quinuclidines Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. J Med Chem 1996 Jul 19;39(15):2971-9
3-(biphenyl-4-yl)-3-hydroxyquinuclidine  0   *Quinuclidines Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. Biochem Pharmacol 1996 Jun 14;51(11):1477-87
3-(biphenyl-4-yl)quinuclidine  0   *Quinuclidines Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. Biochem Pharmacol 1996 Jun 14;51(11):1477-87
TAN 1607A  0   *Tricarboxylic Acids *Bicyclo Compounds, Heterocyclic Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. Biochem Biophys Res Commun 1996 Feb 15;219(2):515-520
squalestatin 3  142505-92-8   *Tricarboxylic Acids *Bicyclo Compounds, Heterocyclic Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. Phytochemistry 1995 Mar;38(5):1137-41
squalestatin 2  142505-91-7   *Tricarboxylic Acids *Bicyclo Compounds, Heterocyclic Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. Phytochemistry 1995 Mar;38(5):1137-41
CrtM protein, Staphylococcus aureus  EC 1.3.-   *Bacterial Proteins *Farnesyl-Diphosphate Farnesyltransferase. J Bacteriol 1994 Dec;176(24):7719-26
zaragozic acid D(2)  155179-15-0   *Tricarboxylic Acids *Bicyclo Compounds, Heterocyclic Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. J Nat Prod 1993 Nov;56(11):1923-9
zaragozic acid D  155179-14-9   *Tricarboxylic Acids *Bicyclo Compounds, Heterocyclic Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. J Nat Prod 1993 Nov;56(11):1923-9
N-homogeranyl-N-methyl-N'-farnesylformamidine  147315-58-0   *Amidines Farnesol/*analogs & derivatives Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. J Med Chem 1993 Mar 5;36(5):631-2
zaragozic acid C  137681-56-2   *Bicyclo Compounds, Heterocyclic Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. Proc Natl Acad Sci U S A 1993 Jan 1;90(1):80-4
zaragozic acid B  146389-61-9 L-glycero-D-altro-Pentadec-14-en-7-ulo-7,4-furanosonic acid, 2,7-anhydro-3,4-di-C-carboxy-8,9,10,12,13,14,15-heptadeoxy-10,12-dimethyl-15-phenyl-, 5-(6,12-tetradecadienoate), (5(6E,12E),7S,10xi,11xi,12xi)  *Bicyclo Compounds, Heterocyclic Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors. Proc Natl Acad Sci U S A 1993 Jan 1;90(1):80-4
squalestatin 1  142561-96-4   *Tricarboxylic Acids *Bicyclo Compounds, Heterocyclic Farnesyl-Diphosphate Farnesyltransferase/antagonists & inhibitors.
Pharma Action Anticholesteremic Agents ; Antifungal Agents ; Enzyme Inhibitors 		J Biol Chem 1992 Jun 15;267(17):11705-8

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