Target Information
Target General Infomation | |||||
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Target ID |
T64081
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Former ID |
TTDC00065
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Target Name |
Farnesyltransferase
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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
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Target Type |
Discontinued
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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.
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BioChemical Class |
Alkyl aryl transferase
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Target Validation |
T64081
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EC Number |
EC 2.5.1.59
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Drugs and Mode of Action | |||||
Drug(s) | ABT-839 | Drug Info | Terminated | Non-small cell lung cancer | [547261] |
AZD3409 | Drug Info | Terminated | Solid tumours | [542931], [547315] | |
L-731735 | Drug Info | Terminated | Cancer | [545288] | |
L-745631 | Drug Info | Terminated | Cancer | [546335] | |
MANUMYCIN A | Drug Info | Terminated | Discovery agent | [546113] | |
RPR-113829 | Drug Info | Terminated | Discovery agent | [546523] | |
RPR-114334 | Drug Info | Terminated | Discovery agent | [546522] | |
SCH-44342 | Drug Info | Terminated | Discovery agent | [546334] | |
Inhibitor | (Z)-2-Methyl-3-tetradecyl-but-2-enedioic acid | Drug Info | [534466] | ||
ABT-839 | Drug Info | [526584] | |||
ACTINOPLANIC ACID A | Drug Info | [534466] | |||
ALPHA-HYDROXYFARNESYLPHOSPHONIC ACID | Drug Info | [551374] | |||
AZD3409 | Drug Info | [536218], [536277], [536283] | |||
BMS-404683 | Drug Info | [527568] | |||
CLAVARINONE | Drug Info | [534739] | |||
FARNESYL | Drug Info | [551374] | |||
GERANYLGERANYL DIPHOSPHATE | Drug Info | [551374] | |||
L-731735 | Drug Info | [534664] | |||
L-745631 | Drug Info | [534466] | |||
MANUMYCIN A | Drug Info | [526603] | |||
PB-27 | Drug Info | [527568] | |||
PB-80 | Drug Info | [527568] | |||
PB-81 | Drug Info | [527568] | |||
PD-83176 | Drug Info | [534307] | |||
Pseudopeptide derivative | Drug Info | [551289] | |||
RPR-113829 | Drug Info | [534405] | |||
RPR-114334 | Drug Info | [534405] | |||
SCH-44342 | Drug Info | [525518] | |||
Pathways | |||||
References | |||||
Ref 542931 | (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 545288 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002714) | ||||
Ref 546113 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006417) | ||||
Ref 546334 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007534) | ||||
Ref 546335 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007537) | ||||
Ref 546522 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008739) | ||||
Ref 546523 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008741) | ||||
Ref 525518 | J Med Chem. 1999 Jun 17;42(12):2125-35.Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships. | ||||
Ref 526584 | Bioorg Med Chem Lett. 2003 Apr 7;13(7):1359-62.Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. | ||||
Ref 526603 | Bioorg Med Chem Lett. 2003 May 5;13(9):1523-6.A novel metal-chelating inhibitor of protein farnesyltransferase. | ||||
Ref 527568 | J Med Chem. 2005 Jun 2;48(11):3704-13.Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. | ||||
Ref 534307 | J Med Chem. 1997 Jan 17;40(2):192-200.Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase. | ||||
Ref 534405 | J Med Chem. 1997 Jun 6;40(12):1763-7.Novel conformationally extended naphthalene-based inhibitors of farnesyltransferase. | ||||
Ref 534664 | J Med Chem. 1998 Jul 2;41(14):2651-6.N-Arylalkyl pseudopeptide inhibitors of farnesyltransferase. | ||||
Ref 534739 | J 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 536218 | Quantification 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 536277 | Radiosensitizing 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 536283 | AZD3409 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. |
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