Structures of BRAF-MEK1-14-3-3 sheds light on drug discovery.

Signal Transduct Target Ther

State Key Laboratory of Biotherapy, Cancer Center, West China Hospital, Sichuan University and Collaborative Innovation Center for Biotherapy, Chengdu, 610041 China.

Published: January 2021

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6908589PMC
http://dx.doi.org/10.1038/s41392-019-0096-zDOI Listing

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Structures of BRAF-MEK1-14-3-3 sheds light on drug discovery.

Signal Transduct Target Ther

January 2021

State Key Laboratory of Biotherapy, Cancer Center, West China Hospital, Sichuan University and Collaborative Innovation Center for Biotherapy, Chengdu, 610041 China.

View Article and Find Full Text PDF

RAF family kinases are RAS-activated switches that initiate signalling through the MAP kinase cascade to control cellular proliferation, differentiation and survival. RAF activity is tightly regulated and inappropriate activation is a frequent cause of cancer; however, the structural basis for RAF regulation is poorly understood at present. Here we use cryo-electron microscopy to determine autoinhibited and active-state structures of full-length BRAF in complexes with MEK1 and a 14-3-3 dimer.

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