Hitting KRAS When It's Down

被引：10
作者：
Gabizon, Ronen [1 ]
London, Nir [1 ]
机构：
[1] Weizmann Inst Sci, Dept Organ Chem, IL-7600001 Rehovot, Israel
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2020年 / 63卷 / 13期
关键词：
INHIBITORS;
D O I：
10.1021/acs.jmedchem.0c00785
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
KRAS, one of the most prevalent oncogenes and sought-after anticancer targets, has eluded chemists for decades until an irreversible covalent strategy targeting a specific mutation (G12C) paved the way for the first KRAS inhibitors to reach the clinic. MRTX849 is one such clinical candidate with promising initial results in patients harboring the mutation. The impressive optimization story of MRTX849 highlights challenges and solutions in the development of covalent drugs, including the use of an alpha-fluoroacrylamide electrophile.
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收藏
页码：6677 / 6678
页数：2
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