Therapeutic Targets Database
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TTD Target ID: TTDR01076

Target Information
NameProtein farnesyltransferase beta subunit    
Type of targetResearch target    
SynonymsCAAX farnesyltransferase beta subunit    
FTase-beta    
RAS proteins prenyltransferase beta    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[1]
BioChemical ClassTransferases transferring alkyl or aryl groups    
EC NumberEC 2.5.1.58
UniProt IDP49356
PDB Structure1JCQ; 1LD7; 1LD8; 1MZC; 1S63; 1SA4; 1TN6; 2F0Y; 2H6F; 2H6G; 2H6H; 2H6I; 2IEJ; 3E37.    
FunctionCatalyzes the transfer of a farnesyl moiety from farnesyl pyrophosphate to a cysteine at the fourth position from the c-terminus of several proteins. The beta subunit is responsible for peptide-binding.    
SequenceMASPSSFTYYCPPSSSPVWSEPLYSLRPEHARERLQDDSVETVTSIEQAKVEEKIQEVFS SYKFNHLVPRLVLQREKHFHYLKRGLRQLTDAYECLDASRPWLCYWILHSLELLDEPIPQ IVATDVCQFLELCQSPEGGFGGGPGQYPHLAPTYAAVNALCIIGTEEAYDIINREKLLQY LYSLKQPDGSFLMHVGGEVDVRSAYCAASVASLTNIITPDLFEGTAEWIARCQNWEGGIG GVPGMEAHGGYTFCGLAALVILKRERSLNLKSLLQWVTSRQMRFEGGFQGRCNKLVDGCY SFWQAGLLPLLHRALHAQGDPALSMSHWMFHQQALQEYILMCCQCPAGGLLDKPGKSRDF YHTCYCLSGLSIAQHFGSGAMLHDVVLGVPENALQPTHPVYNIGPDKVIQATTYFLQKPV PGFEELKDETSAEPATD
Target ValidationClick to Find Target Validation Information.    
Inhibitor (Z)-2-Methyl-3-tetradecyl-but-2-enedioic acid[2]
A-313326[3]
ABT-839[3]
ACTINOPLANIC ACID A[2]
ALPHA-HYDROXYFARNESYLPHOSPHONIC ACID[4]
ARTEMINOLIDE[5]
BMS-214662[6]
BMS-316810[7]
BMS-404683[8]
CLAVARINONE[9]
CYLINDROL A[2]
FARNESYL[4]
FARNESYL DIPHOSPHATE[4]
FUSIDIENOL[5]
GERANYLGERANYL DIPHOSPHATE[4]
H-SMGLPCVVM-OH[10]
L-731735[2]
L-739749[2]
L-739750[2]
L-745631[2]
L-778123[11]
MANUMYCIN A[12]
PB-27[8]
PB-80[8]
PB-81[8]
PD-83176[13]
PREUSSOMERIN[2]
Prenyl pyrophosphate analogue[14]
Prenyl pyrophosphate analogue[14]
Prenyl pyrophosphate analogue[14]
Prenyl pyrophosphate analogue[14]
Prenyl pyrophosphate analogue[14]
Pseudopeptide derivative[15]
Pseudopeptide derivative[15]
RPR-113829[16]
RPR-114334[16]
SCH-44342[2]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. To Reference
Ref 2J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target. To Reference
Ref 3Bioorg Med Chem Lett. 2005 Jan 3;15(1):153-8.Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase. To Reference
Ref 4Berman 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 5J Med Chem. 2002 Mar 28;45(7):1460-5.Modeling of binding modes and inhibition mechanism of some natural ligands of farnesyl transferase using molecular docking. To Reference
Ref 6J Med Chem. 2004 Apr 8;47(8):1869-78.Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy? To Reference
Ref 7Bioorg Med Chem Lett. 2005 Apr 1;15(7):1895-9.Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors. To Reference
Ref 8J Med Chem. 2005 Jun 2;48(11):3704-13.Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. To Reference
Ref 9J Med Chem. 1998 Nov 5;41(23):4492-501.Clavaric acid and steroidal analogues as Ras- and FPP-directed inhibitors of human farnesyl-protein transferase. To Reference
Ref 10Bioorg Med Chem Lett. 2003 Aug 4;13(15):2583-6.Improvement of biological activity and proteolytic stability of peptides by coupling with a cyclic peptide. To Reference
Ref 11Bioorg Med Chem Lett. 2001 Feb 26;11(4):537-40.Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase. To Reference
Ref 12Bioorg Med Chem Lett. 2003 May 5;13(9):1523-6.A novel metal-chelating inhibitor of protein farnesyltransferase. To Reference
Ref 13J Med Chem. 1997 Jan 17;40(2):192-200.Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase. To Reference
Ref 14Bioorg. Med. Chem. Lett. 7(16):2125-2130 (1997) To Reference
Ref 15Bioorg. Med. Chem. Lett. 5(22):2677-2682 (1995) To Reference
Ref 16J Med Chem. 1997 Jun 6;40(12):1763-7.Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase. To Reference



 

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