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Dabrafenib: the New Inhibitor of Hyperactive B-RAF Kinase

Publication at Third Faculty of Medicine |
2012

Abstract

The B-RAF kinase is among major targets of biological therapy of cancer. B-RAF acts in the MAP kinase pathway, being activated by any of the RAS G-proteins.

Hyperactive B-RAF is typically detected in chemoresistant and radioresistant malignant metastatic melanoma. In this study, we focus on the reversible ATP-competitive inhibitor dabrafenib (GSK-2118436), which is now in phase III clinical trial for use in subjects with various cancers expressing hyperactive B-RAF.