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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Recent Advances in the Research and Development of B-Raf Inhibitors

Author(s): Hui-Fang Li, Yadong Chen, Sha-Sha Rao, Xiu-Mei Chen, Hai-Chun Liu, Ji-Hong Qin, Wei-Fang Tang, Yue-Wang, Xiang Zhou and Tao Lu

Volume 17 , Issue 16 , 2010

Page: [1618 - 1634] Pages: 17

DOI: 10.2174/092986710791111242

Price: $65


Oncogenic B-Raf has been identified in a variety of cancers with high incidence, especially in malignant melanoma and thyroid cancer. Most B-Raf mutations elicit elevated kinase activity and the constitutive activation of Ras/Raf/MEK/ERK pathway, which induces proliferation and promotes malignant transformation. Therefore, B-Raf inhibitors, targeting B-Raf or mutated B-Raf, have received increasing momentum in oncology drug discovery arena. This review focuses on the diverse small-molecule inhibitors of B-Raf kinase recently reported in the literature, including those currently in clinical and preclinical phase. They are described as two categories, type I or type II kinase inhibitors, based on their different mechanism of action with active or inactive conformations of the B-Raf kinase derived from the available crystal structures or molecular docking analysis. A particular emphasis is placed on their binding modes and the structure-activity relationship (SAR) of each chemical structure class.

Keywords: B-Raf, B-RafV600E, B-Raf kinase inhibitors, binding mode, SAR, mechanism of action

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