期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 55, 期 52, 页码 15982-15988出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201608270
关键词
computational chemistry; inhibitors; medicinal chemistry; peptides; Ras
Owing to their high occurrence rate across many human cancers and their lack of druggability so far, mutant forms of the signaling protein Ras are currently among the most attractive (and elusive) oncology targets. This strong appeal explains the sustained effort in the field, and the ensuing progress has rekindled optimism regarding the discovery of Ras inhibitors. In this Minireview, we discuss the most recent advances towards irreversible inhibitors, and highlight approaches to inhibitors of Ras-effector interactions that have been overshadowed by the current focus on direct Ras inhibition. At the same time, we provide a critical assessment from a medicinal chemistry perspective.
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