Advances in the research and development of B-Raf inhibitors

DONG Gaochao; ZHOU Xiang; TANG Weifang; LU Tao

doi:10.11665/j.issn.1000-5048.20140101

Journal of China Pharmaceutical University > 2014 > 45(1): 1-9. > DOI: 10.11665/j.issn.1000-5048.20140101

DONG Gaochao, ZHOU Xiang, TANG Weifang, LU Tao. Advances in the research and development of B-Raf inhibitors[J]. Journal of China Pharmaceutical University, 2014, 45(1): 1-9. DOI: 10.11665/j.issn.1000-5048.20140101

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Advances in the research and development of B-Raf inhibitors

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Abstract

Oncogenic B-Raf has been identified in a variety of cancers with high incidence, especially in malignant melanoma and thyroid cancer. In 2011, selective B-Raf kinase inhibitor vemurafenib was approved by FDA, and that stimulated increasing interest in B-Raf inhibitors as anticancer agents. Through analyzing the X-ray crystal structure of vemurafenib bound to B-Raf kinase, new classification of B-Raf kinase inhibitors was proposed. This review focuses on diverse small-molecule inhibitors of B-Raf kinase published in protein data bank(PDB)from 2011 to date based on the new classification. The binding modes and structure-activity relationship(SAR)as well as the future development of these inhibitors are discussed.
- B-Raf kinase,
- B-Raf kinase inhibitor,
- classification

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