RAF family | Enzymes | IUPHAR/BPS Guide to PHARMACOLOGY

RAF family C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Enzymes

A-Raf (A-Raf proto-oncogene, serine/threonine kinase) Show summary »« Hide summary More detailed page

Target Id

1933

Nomenclature

A-Raf proto-oncogene, serine/threonine kinase

Common abbreviation

A-Raf

Previous and unofficial names

Genes

ARAF (Hs), Araf (Mm), Araf (Rn)

Ensembl ID

ENSG00000078061 (Hs), ENSMUSG00000001127 (Mm), ENSRNOG00000010838 (Rn)

UniProtKB AC

P10398 (Hs), P04627 (Mm), P14056 (Rn)

EC number

2.7.11.1

B-Raf (B-Raf proto-oncogene, serine/threonine kinase) C Show summary »« Hide summary More detailed page

KSR (kinase suppressor of ras 1) Show summary »« Hide summary More detailed page

KSR2 (kinase suppressor of ras 2) Show summary »« Hide summary More detailed page

c-Raf (Raf-1 proto-oncogene, serine/threonine kinase) C Show summary »« Hide summary More detailed page

Target Id

2184

Nomenclature

Raf-1 proto-oncogene, serine/threonine kinase

Common abbreviation

c-Raf

Previous and unofficial names

RAF proto-oncogene serine/threonine-protein kinase | Raf-1 proto-oncogene

Genes

RAF1 (Hs), Raf1 (Mm), Raf1 (Rn)

Ensembl ID

ENSG00000132155 (Hs), ENSMUSG00000000441 (Mm), ENSRNOG00000010153 (Rn)

UniProtKB AC

P04049 (Hs), Q99N57 (Mm), P11345 (Rn)

EC number

2.7.11.1

Selective inhibitors

GW5074 pIC₅₀ 8.1 [1]

References

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1. Chin PC, Liu L, Morrison BE, Siddiq A, Ratan RR, Bottiglieri T, D'Mello SR. (2004) The c-Raf inhibitor GW5074 provides neuroprotection in vitro and in an animal model of neurodegeneration through a MEK-ERK and Akt-independent mechanism. J. Neurochem., 90 (3): 595-608. [PMID:15255937]

2. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

3. Hansen JD, Grina J, Newhouse B, Welch M, Topalov G, Littman N, Callejo M, Gloor S, Martinson M, Laird E et al.. (2008) Potent and selective pyrazole-based inhibitors of B-Raf kinase. Bioorg. Med. Chem. Lett., 18 (16): 4692-5. [PMID:18676143]

4. Horbert R, Pinchuk B, Davies P, Alessi D, Peifer C. (2015) Photoactivatable Prodrugs of Antimelanoma Agent Vemurafenib. ACS Chem. Biol., 10 (9): 2099-107. [PMID:26061392]

5. Laquerre S, Arnone M, Moss K, Yang J, Fisher K, Kane-Carson LS, Smitheman K, Ward J, Heidrich B, Rheault T et al. (2009) Abstract B88: A selective Raf kinase inhibitor induces cell death and tumor regression of human cancer cell lines encoding B-RafV600E mutation. Molecular Cancer Therapeutics, 8 (12) Meeting Abstract.

6. Wang X, Kim J. (2012) Conformation-specific effects of Raf kinase inhibitors. J. Med. Chem., 55 (17): 7332-41. [PMID:22808911]

7. Zambon A, Niculescu-Duvaz I, Niculescu-Duvaz D, Marais R, Springer CJ. (2012) Small molecule inhibitors of BRAF in clinical trials. Bioorg. Med. Chem. Lett., 22 (2): 789-92. [PMID:22222036]

How to cite this family page

Database page citation:

RAF family. Accessed on 16/02/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=610.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Marrion NV, Peters JA, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2017) The Concise Guide to PHARMACOLOGY 2017/18: Enzymes. Br J Pharmacol. 174 Suppl 1: S272-S359.