Discovery of a Novel EGFR PROTAC Degrader against C797S Resistance Mutation with Potent Antitumor Efficacy in NSCLC Treatment

C797S mutation is the predominant resistance mechanism for the third-generation EGFR inhibitor osimertinib in nonsmall cell lung cancer (NSCLC). To overcome this drug resistance, a novel class of EGFR<sup>C797S</sup> PROTAC degraders was developed in human NSCLC models. <b>9ea</...

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主要作者:	Xiaoxue Wang (311457) (author)
其他作者:	Cheng Wang (102692) (author), Yakun Ma (4801680) (author), Yongjun Piao (3554345) (author), Yi Shi (169113) (author), Shuang Yang (64650) (author), Jia Li (160557) (author), Yan Fan (575147) (author)
出版:	2025
主题:	Biophysics Biochemistry Cell Biology Genetics Molecular Biology Pharmacology Biotechnology Cancer Science Policy Infectious Diseases Biological Sciences not elsewhere classified Chemical Sciences not elsewhere classified mechanistic studies revealed exhibited good selectivity predominant resistance mechanism c797s resistance mutation 9 ± 1 1 ± 6 potent antitumor efficacy selectively induced egfr main egfr mutants human nsclc models max </ sub c797s </ sup 9ea </ b 50 </ sub demonstrating potent degradation drug resistance 1 nm 50 mg >< sub selective egfr egfr mutant downregulated egfr tumor tissue protac degraders protac degrader nsclc ). novel class lead compound findings suggest driven nsclc dependent manner associated transcriptome 5 %).
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Discovery of a Novel EGFR PROTAC Degrader against C797S Resistance Mutation with Potent Antitumor Efficacy in NSCLC Treatment

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