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Article

Discovery of Isoform-Selective Akt3 Degraders Overcoming Osimertinib-Induced Resistance in Non-Small Cell Lung Cancer Cells.

Journal of medicinal chemistry - 27 Oct 2022

Xu Fang, Zhang Xin, Chen Zhipeng, He Sheng, Guo Jing, Yu Lei, Wang Yongjin, Hou Caiyun, Ai-Furas Hawaa, Zheng Zongyao, Smaill Jeff B, Patterson Adam V, Zhang Zhi-Min, Chen Liang, Ren Xiaomei, Ding Ke

Abstract excerpt

EGFR inhibitor therapies have brought significant benefit to NSCLC patients. However, all patients gradually progress to acquired resistance via diverse mechanisms. Akt3 overexpression but not Akt1/2 is one of the found molecular events that mediate osimertinib (1) resistance in NSCLC patients. Here, we report 12l as the first bona fide isoform-selective Akt3 degrader which potently induced proteasomal...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 36173763
DOI: 10.1021/acs.jmedchem.2c01246

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