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farnesyltransferase, CAAX box, beta

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Target not currently curated in GtoImmuPdb

Target id: 2826

Nomenclature: farnesyltransferase, CAAX box, beta

Abbreviated Name: FNTB

Family: 2.5.1.58 Protein farnesyltransferase

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 437 14q23.3 FNTB farnesyltransferase, CAAX box, beta
Mouse - 437 12 33.73 cM Fntb farnesyltransferase, CAAX box, beta
Rat - 437 6q24 Fntb farnesyltransferase, CAAX box, beta
Previous and Unofficial Names Click here for help
farnesyltransferase
Database Links Click here for help
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
FTI 276 Small molecule or natural product Primary target of this compound Hs Inhibition 9.3 pIC50 6
pIC50 9.3 (IC50 5x10-10 M) [6]
tipifarnib Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 9.1 pIC50 1-2
pIC50 9.1 (IC50 8.6x10-10 M) [1-2]
Description: Inhibition of [3H]FPP incorporation into biotinylated laminB peptide by farnesyltransferase protein complex
BMS-214662 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.9 pIC50 3
pIC50 8.9 (IC50 1.35x10-9 M) [3]
LB42908 Small molecule or natural product Primary target of this compound Hs Inhibition 8.6 – 9.1 pIC50 5
pIC50 8.6 – 9.1 (IC50 2.4x10-9 – 9x10-10 M) [5]
Description: Measured as inhibition of FTase transfer of [3H]-farnesylpyrophosphate (FPP) to HRAS (0.9nM) or NRAS (2.4nM)
L-739,750 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.7 pIC50 4
pIC50 8.7 (IC50 1.8x10-9 M) [4]
Inhibitor Comments
Note that for farnesyltransferase inhibitors we map the ligand interaction to the beta subunit, although the actual active site forms in the centre of the beta subunit overlapped by the alpha subunit.
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes
GO:0034097 response to cytokine IMP

References

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1. Angibaud P, Bourdrez X, Devine A, End DW, Freyne E, Ligny Y, Muller P, Mannens G, Pilatte I, Poncelet V et al.. (2003) 5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors. Bioorg. Med. Chem. Lett., 13 (9): 1543-7. [PMID:12699751]

2. End DW, Smets G, Todd AV, Applegate TL, Fuery CJ, Angibaud P, Venet M, Sanz G, Poignet H, Skrzat S et al.. (2001) Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro. Cancer Res., 61 (1): 131-7. [PMID:11196150]

3. Hunt JT, Ding CZ, Batorsky R, Bednarz M, Bhide R, Cho Y, Chong S, Chao S, Gullo-Brown J, Guo P et al.. (2000) Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity. J. Med. Chem., 43 (20): 3587-95. [PMID:11020273]

4. Kohl NE, Wilson FR, Mosser SD, Giuliani E, deSolms SJ, Conner MW, Anthony NJ, Holtz WJ, Gomez RP, Lee TJ et al.. (1994) Protein farnesyltransferase inhibitors block the growth of ras-dependent tumors in nude mice. Proc. Natl. Acad. Sci. U.S.A., 91 (19): 9141-5. [PMID:8090782]

5. Lee H, Lee J, Lee S, Shin Y, Jung W, Kim JH, Park K, Kim K, Cho HS, Ro S et al.. (2001) A novel class of highly potent, selective, and non-peptidic inhibitor of Ras farnesyltransferase (FTase). Bioorg. Med. Chem. Lett., 11 (23): 3069-72. [PMID:11714612]

6. Lerner EC, Qian Y, Blaskovich MA, Fossum RD, Vogt A, Sun J, Cox AD, Der CJ, Hamilton AD, Sebti SM. (1995) Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras-Raf complexes. J. Biol. Chem., 270 (45): 26802-6. [PMID:7592920]

How to cite this page

2.5.1.58 Protein farnesyltransferase: farnesyltransferase, CAAX box, beta. Last modified on 13/08/2015. Accessed on 28/11/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2826.