Target intelligence / Profile preview

Proto-oncogene protein B-Raf (BRAF)

Target
BRAF
Molecular classification
Enzyme, Protein Kinase, Serine/threonine kinase
01

Overview

BRAF is a serine/threonine protein kinase that functions as a key component of the RAF family and regulates the MAP kinase/ERK signaling pathway. It plays a crucial role in cell division, differentiation, migration, secretion, and apoptosis. Mutations in BRAF, particularly V600E, are implicated in various cancers and developmental syndromes, making it an important therapeutic target. Inhibitors like vemurafenib and dabrafenib are used in treating late-stage melanoma with V600E mutations.

Other names
Serine/threonine-protein kinase B-Rafv-Raf murine sarcoma viral oncogene homolog B
02

Mechanism of action

Inhibition of BRAF kinase activity, specifically mutant forms like V600E

03

Biological functions

Signal transductionCell proliferationCell differentiationCell migrationSecretionApoptosisRegulation of MAP kinase/ERK signaling pathway
04

Disease associations

CancerRASopathiesMelanomaNon-Hodgkin lymphomaColorectal cancerThyroid carcinomaNon-small cell lung carcinoma (NSCLC)Hairy cell leukemiaNoonan syndrome (NS)Cardio-facio-cutaneous syndrome (CFC)Costello syndrome
05

Safety considerations

Resistance to BRAF inhibitors can developParadoxical activation of MAPK pathway in wild-type BRAF cellsNot effective against all BRAF mutation types
06

Interacting drugs

Vemurafenib

1 more in the full profile.

07

Biomarkers

BRAF V600E mutation (for patient selection in melanoma and other cancers)

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