Journal
CURRENT ONCOLOGY REPORTS
Volume 12, Issue 3, Pages 146-152Publisher
SPRINGER
DOI: 10.1007/s11912-010-0095-2
Keywords
Malignant melanoma; B-RAF inhibitors
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Funding
- NCI NIH HHS [K24 CA097588] Funding Source: Medline
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Immunotherapy and chemotherapy benefit few patients with metastatic melanoma, and even fewer experience durable survival benefit. These poor results come from treating melanoma as a single homogeneous disease. Recently, it has been shown that targeting activated tyrosine kinases (oncogenes) can mediate striking clinical benefits in several cancers. In 2002, a mutation at the V600E amino acid of the BRAF serine/threonine kinase was described as present in over 50% of melanomas. The mutation appeared to confer a dependency by the melanoma cancer cell on its activation of the MAP kinase pathway. The frequency and specificity of this mutation (95% at V600E of BRAF) suggests that it may be a potential target for therapy, and recent results with one inhibitor, PLX4032/RG7204, bare this out. This review updates the status of BRAF inhibitors in melanoma and what may be on the horizon.
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