farnesyltransferase, CAAX box, beta

Target id: 2826

Nomenclature: farnesyltransferase, CAAX box, beta

Abbreviated Name: FNTB

Family: 2.5.1.58 Protein farnesyltransferase

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for farnesyltransferase, CAAX box, beta in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 437 14q23.3 FNTB farnesyltransferase, CAAX box, beta
Mouse - 437 12 C3 Fntb farnesyltransferase, CAAX box, beta
Rat - 437 6q24 Fntb farnesyltransferase, CAAX box, beta
Previous and Unofficial Names
farnesyltransferase
Database Links
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
FTI 276 Hs Inhibition 9.3 pIC50 6
pIC50 9.3 (IC50 5x10-10 M) [6]
tipifarnib 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 Hs Inhibition 8.9 pIC50 3
pIC50 8.9 (IC50 1.35x10-9 M) [3]
LB42908 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 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.

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 23/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2826.