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Target intelligence / Profile preview
Serine/threonine-protein kinase BRAF (BRAF)
- Target
- BRAF
- Molecular classification
- Enzyme, Protein kinase, Serine/threonine kinase
01
Overview
Serine/threonine-protein kinase BRAF (B-Raf) is a key component of the RAS/MAPK signaling pathway, regulating cell division, differentiation, migration, and apoptosis. Mutations, particularly V600E, lead to constitutive activation and are implicated in various cancers, making it an important therapeutic target. Several selective inhibitors have been developed for clinical use.
- Other names
- B-Rafv-raf murine sarcoma viral oncogene homolog B1BRAF1
02
Mechanism of action
Selective inhibition of mutant BRAF kinase activity, particularly V600E
03
Biological functions
Signal transductionCell proliferationCell differentiationCell migrationApoptosisRegulation of MAPK pathway
04
Disease associations
CancerMelanomaColorectal cancerThyroid carcinomaNon-small cell lung carcinomaHairy cell leukemiaRASopathiesNoonan syndromeCardio-facio-cutaneous syndrome (CFC)Costello syndrome
05
Safety considerations
Development of resistanceParadoxical activation of MAPK pathway in BRAF wild-type cells leading to increased proliferationCutaneous squamous cell carcinomaCardiotoxicity
06
Interacting drugs
Vemurafenib
2 more in the full profile.
07
Biomarkers
BRAF V600E mutationBRAF mutations
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