Allele-Specific Mechanisms of Activation of MEK1 Mutants Determine Their Properties

MEK1 突变体的等位基因特异性激活机制决定了其特性

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作者:Yijun Gao, Matthew T Chang, Daniel McKay, Na Na, Bing Zhou, Rona Yaeger, Neilawattie M Torres, Keven Muniz, Matthias Drosten, Mariano Barbacid, Giordano Caponigro, Darrin Stuart, Henrik Moebitz, David B Solit, Omar Abdel-Wahab, Barry S Taylor, Zhan Yao, Neal Rosen

Significance

Mutants with which MEK1 mutants coexist and their sensitivity to inhibitors are determined by allele-specific properties. This study shows the importance of functional characterization of mutant alleles in single oncogenes and identifies a new class of MEK1 mutants, insensitive to current MEK1 inhibitors but treatable with a new ATP-competitive inhibitor. Cancer Discov; 8(5); 648-61. ©2018 AACR.See related commentary by Maust et al., p. 534This article is highlighted in the In This Issue feature, p. 517.

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