Targeting mutant KRAS

被引：16

作者：

Erlanson, Daniel A. ^{[1
]}

Webster, Kevin R. ^{[1
]}

机构：

[1] Frontier Med Corp, 151 Oyster Point Blvd,2nd Floor, San Francisco, CA 94080 USA

来源：

CURRENT OPINION IN CHEMICAL BIOLOGY | 2021年 / 62卷

关键词：

KRAS;   G12C; G12D; Covalent drugs; Precision oncology; Fragment -based drug discovery; AMG; 510; INHIBITORS; KRAS(G12C); DISCOVERY;

D O I：

10.1016/j.cbpa.2021.02.010

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The protein KRAS has for decades been considered a holy grail of cancer drug discovery. For most of that time, it has also been considered undruggable. Since 2018, five compounds have entered the clinic targeting a single mutant form of KRAS, G12C. Here, we review each of these compounds along with additional approaches to targeting this and other mutants. Remaining challenges include expanding the identification of inhibitors to a broader range of known mutants and to con -formations of the protein more likely to avoid development of resistance.

引用

页码：101 / 108

页数：8

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