Therapeutic Targets Database
BIDD Pharmainformatics Databases


TTD Target ID: TTDS00372

Target Information
NameFarnesyl pyrophosphate synthetase    
Type of targetSuccessful target    
SynonymsFPP synthase    
FPP synthetase    
Farnesyl diphosphate synthase    
Farnesyl diphosphate synthetase    
Farnesyl pyrophosphate synthase    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
Chagas' disease
[ICD9: 086   ICD10: B57]
[ICD9: 272.0   ICD10: E78.0]
Leishmania infections
[ICD9: 001-139, 296.0, 296.4, 296.6   ICD10: A00-B99, F30]
Myeloma disease
[ICD9: 203.0   ICD10: C90.0]
Osteoporosis, unspecified
[ICD9: 733.0   ICD10: M80-M81]
Skeletal disorders[7]
Toxoplasma infections
[ICD9: 001-139   ICD10: A00-B99]
Trypanosomatid infections
[ICD9: 001-139   ICD10: A00-B99]
Drug(s)AlendronateApprovedOsteoporosis and Paget's disease[10][4][11][6]
IbandronateApprovedOsteoporosis in post-menopausal women[12]
Pamidronate disodiumApprovedOsteoporosis[10]
RisedronateApprovedPaget's disease[9]
Zoledronic acidApprovedPostmenopausal osteoporosis[15][16]
EC NumberEC
PathwayBiosynthesis of steroids
Metabolic pathways
Terpenoid biosynthesis
UniProt IDP14324
PDB Structure1YQ7; 1YV5; 1ZW5; 2F7M; 3DYF; 3DYG; 3DYH; 3EFQ.    
FunctionCatalyzes the sequential condensation of isopentenyl pyrophosphate with the allylic pyrophosphates, dimethylallyl pyrophosphate, and then with the resultant geranylpyrophosphate to the ultimate product farnesyl pyrophosphate.    
Target ValidationClick to Find Target Validation Information.    
Inhibitor (1-hydroxy-1-phosphono-heptyl)-phosphonic acid[17]
(biphenyl-3-ylamino)methylenediphosphonic acid[18]
1- (but-2-ylamino)ethyl 1,I-bisphosphonic acid[17]
1-[ (cyclohexylamino)ethyl]-1,1-bisphosphonicacid[17]
1-[ (n-but-1-ylamino)ethyl]-1,1-bisphosphonic acid[17]
1-[ (n-hex-1-ylamino)ethyl]-1,1-bisphosphonic acid[17]
1-[ (n-oct-1-ylamino)ethyl]-1,1-bisphosphonic acid[17]
1-[ (prop-1-ylamino)ethyl]-1,1-bisphosphonic acid[17]
1-[ (prop-2-ylamino)ethyl]-1,1-bisphosphonicacid[17]
1-[ (tert-butylamino)ethyl]-1,1-bisphosphonicacid[17]
Bisphosphonates alendronate[2]
Dimethylallyl Diphosphate[19]
Farnesyl pyrophosphate[20]
Geranyl Diphosphate[21]
Isopentyl Pyrophosphate[21]
Pamidronate disodium[10]
Piridronic acid[22]
Zoledronic acid[15][16]
[2- (6-Chloro-purin-9-yl)ethyl]-bisphosphonic acid[24]
[2- (Benzoimidazol-1-yl)ethyl]-bisphosphonic acid[24]
[2- (Imidazol-1-yl)ethyl]-bisphosphonic acid[24]
[2- (Imidazol-2-yl-thio)ethyl]-bisphosphonic acid[24]
[2- (Purin-9-yl)ethyl]-bisphosphonic acid[24]
[2- (Pyrazol-1-yl)ethyl]-bisphosphonic acid[24]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Cancer metastasis therapeutic targets and drug discovery: emerging small-molecule protein kinase inhibitors. Expert Opin Investig Drugs. 2004 Jan;13(1):1-19. To Reference
Ref 2Bisphosphonates are potent inhibitors of Trypanosoma cruzi farnesyl pyrophosphate synthase. J Biol Chem. 2001 Sep 7;276(36):33930-7. Epub 2001 Jul 2. To Reference
Ref 3Squalene epoxidase as hypocholesterolemic drug target revisited. Prog Lipid Res. 2003 Jan;42(1):37-50. To Reference
Ref 4In vivo activities of farnesyl pyrophosphate synthase inhibitors against Leishmania donovani and Toxoplasma gondii. Antimicrob Agents Chemother. 2002 Mar;46(3):929-31. To Reference
Ref 5How myeloma cells escape bisphosphonate-mediated killing: development of specific resistance with preserved sensitivity to conventional chemotherapeutics. Br J Haematol. 2003 Jul;122(2):202-10. To Reference
Ref 6Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys. 2000 Jan 1;373(1):231-41. To Reference
Ref 7Farnesyl pyrophosphate synthase is the molecular target of nitrogen-containing bisphosphonates. Biochem Biophys Res Commun. 1999 Oct 14;264(1):108-11. To Reference
Ref 8Farnesyl pyrophosphate synthase is an essential enzyme in Trypanosoma brucei. In vitro RNA interference and in vivo inhibition studies. J Biol Chem. 2003 May 9;278(19):17075-83. Epub 2003 Mar 4. To Reference
Ref 9Activity of bisphosphonates against Trypanosoma brucei rhodesiense. J Med Chem. 2002 Jul 4;45(14):2904-14. To Reference
Ref 10Nat Rev Drug Discov. 2003 Jan;2(1):38-51.Knockouts model the 100 best-selling drugs--will they model the next 100? To Reference
Ref 11Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates. J Pharmacol Exp Ther. 2001 Feb;296(2):235-42. To Reference
Ref 12Mechanisms of action of bisphosphonates: similarities and differences and their potential influence on clinical efficacy. Osteoporos Int. 2008 Jun;19(6):733-59. To Reference
Ref 13Detection of nonsterol isoprenoids by HPLC-MS/MS. Anal Biochem. 2008 Aug 30. [Epub ahead of print] To Reference
Ref 14Farnesyl 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. 2008 May 1;18(9):2878-82. Epub 2008 Apr 8. To Reference
Ref 15Pulse treatment with zoledronic acid causes sustained commitment of bone marrow derived mesenchymal stem cells for osteogenic differentiation. Bone. 2009 May;44(5):858-64. Epub 2009 Jan 23. To Reference
Ref 16Zoledronic acid - a multiplicity of anti-cancer action. Curr Med Chem. 2007;14(20):2126-35. To Reference
Ref 17Bioorg Med Chem. 2008 Mar 15;16(6):3283-90. Epub 2007 Dec 10.Synthesis and biological evaluation of 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase. To Reference
Ref 18Bioorg Med Chem. 2008 Oct 1;16(19):8959-67. Epub 2008 Aug 27.Bisphosphonate inhibitors of ATP-mediated HIV-1 reverse transcriptase catalyzed excision of chain-terminating 3'-azido, 3'-deoxythymidine: a QSAR investigation. To Reference
Ref 19Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 20A quantitative structure-activity relationship and pharmacophore modeling investigation of aryl-X and heterocyclic bisphosphonates as bone resorption agents. J Med Chem. 2003 Jul 3;46(14):2932-44. To Reference
Ref 21Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 22J Med Chem. 2008 Apr 10;51(7):2187-95. Epub 2008 Mar 8.Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase. To Reference
Ref 23Identification of a bisphosphonate that inhibits isopentenyl diphosphate isomerase and farnesyl diphosphate synthase. Biochem Biophys Res Commun. 2002 Jan 18;290(2):869-73. To Reference
Ref 24J Med Chem. 2008 Nov 13;51(21):6800-7. Epub 2008 Oct 21.Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a gammadelta-T lymphocytes-mediated activation mechanism. To Reference


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