Target Information

Target General Infomation
Target ID
T64081
Former ID
TTDC00065
Target Name
Farnesyltransferase
Synonyms
CAAX farnesyltransferase; CAAX farnesyltransferase alpha subunit; FTase; FTase-alpha; GGTase-I-alpha; Protein farnesyltransferase alpha subunit; RAS proteins prenyltransferase; RAS proteins prenyltransferase alpha; Type I protein geranyl-geranyltransferasealpha subunit
Target Type
Discontinued
Disease Cancer [ICD9: 140-229; ICD10: C00-C96]
Non-small cell lung cancer [ICD10: C33-C34]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Function
Essential subunit of both the farnesyltransferase and the geranylgeranyltransferase complex. Contributes to the transfer of a farnesyl or geranylgeranyl moiety from farnesyl or geranylgeranyl diphosphate to a cysteine at the fourth position from the C-terminus of several proteins having the C-terminal sequence Cys-aliphatic-aliphatic-X. May positively regulate neuromuscular junction development downstream of MUSK via its function in RAC1prenylation and activation.
BioChemical Class
Alkyl aryl transferase
Target Validation
T64081
EC Number
EC 2.5.1.59
Drugs and Mode of Action
Drug(s) ABT-839 Drug Info Terminated Non-small cell lung cancer [1]
AZD3409 Drug Info Terminated Solid tumours [2], [3]
L-731735 Drug Info Terminated Cancer [4]
L-745631 Drug Info Terminated Cancer [5]
MANUMYCIN A Drug Info Terminated Discovery agent [6]
RPR-113829 Drug Info Terminated Discovery agent [7]
RPR-114334 Drug Info Terminated Discovery agent [8]
SCH-44342 Drug Info Terminated Discovery agent [9]
Inhibitor (Z)-2-Methyl-3-tetradecyl-but-2-enedioic acid Drug Info [10]
ABT-839 Drug Info [11]
ACTINOPLANIC ACID A Drug Info [10]
ALPHA-HYDROXYFARNESYLPHOSPHONIC ACID Drug Info [12]
AZD3409 Drug Info [13], [14], [15]
BMS-404683 Drug Info [16]
CLAVARINONE Drug Info [17]
FARNESYL Drug Info [12]
GERANYLGERANYL DIPHOSPHATE Drug Info [12]
L-731735 Drug Info [18]
L-745631 Drug Info [10]
MANUMYCIN A Drug Info [19]
PB-27 Drug Info [16]
PB-80 Drug Info [16]
PB-81 Drug Info [16]
PD-83176 Drug Info [20]
Pseudopeptide derivative Drug Info [21]
RPR-113829 Drug Info [22]
RPR-114334 Drug Info [22]
SCH-44342 Drug Info [23]
Pathways
KEGG Pathway Terpenoid backbone biosynthesis
Biosynthesis of antibiotics
Reactome Apoptotic cleavage of cellular proteins
Inactivation, recovery and regulation of the phototransduction cascade
WikiPathways Visual phototransduction
Apoptotic execution phase
References
REF 1Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014561)
REF 2(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8027).
REF 3Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015097)
REF 4Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002714)
REF 5Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007537)
REF 6Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006417)
REF 7Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008741)
REF 8Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008739)
REF 9Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007534)
REF 10J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target.
REF 11Bioorg Med Chem Lett. 2003 Apr 7;13(7):1359-62.Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.
REF 12The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 13Quantification of farnesylmethylcysteine in lysates of peripheral blood mononuclear cells using liquid chromatography coupled with electrospray tandem mass spectrometry: pharmacodynamic assay for farnesyl transferase inhibitors. Anal Chem. 2006 Apr 15;78(8):2617-22.
REF 14Radiosensitizing effects of the prenyltransferase inhibitor AZD3409 against RAS mutated cell lines. Cancer Biol Ther. 2006 Sep;5(9):1206-10. Epub 2006 Sep 11.
REF 15AZD3409 inhibits the growth of breast cancer cells with intrinsic resistance to the EGFR tyrosine kinase inhibitor gefitinib. Breast Cancer Res Treat. 2007 May;102(3):275-82. Epub 2006 Sep 27.
REF 16J Med Chem. 2005 Jun 2;48(11):3704-13.Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.
REF 17J 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.
REF 18J Med Chem. 1998 Jul 2;41(14):2651-6.N-Arylalkyl pseudopeptide inhibitors of farnesyltransferase.
REF 19Bioorg Med Chem Lett. 2003 May 5;13(9):1523-6.A novel metal-chelating inhibitor of protein farnesyltransferase.
REF 20J Med Chem. 1997 Jan 17;40(2):192-200.Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase.
REF 21Local constrained shifty pseudopeptides inhibitors of rasfarnesyl transferase, Bioorg. Med. Chem. Lett. 5(22):2677-2682 (1995).
REF 22J Med Chem. 1997 Jun 6;40(12):1763-7.Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase.
REF 23J Med Chem. 1999 Jun 17;42(12):2125-35.Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships.

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