Article
Efficient targeted oncogenic KRASG12C degradation via first reversible-covalent PROTAC.
European journal of medicinal chemistry - 15 Feb 2022
Yang Fang, Wen Yalei, Wang Chaofan, Zhou Yuee, Zhou Yang, Zhang Zhi-Min, Liu Tongzheng, Lu Xiaoyun
Abstract excerpt
KRAS is the most frequently mutated oncogene and plays a predominant role in driving initiation and progression of multiple cancers. Attempts to degrade the oncogene KRASG12C with PROTAC strategy have been considered as an alternative strategy to combate cancers. However, the irreversible PROTACs may compromise the substoichiometric activity to decrease the potency. Herein, we report the development of YF135, the...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.