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Discovery of a miniaturized PROTAC with potent activity and high selectivity.

Bioorganic chemistry - 1 Jul 2023

Gong Lidong, Li Ridong, Gong Jingjing, Ning Xianling, Sun Jiawei, Ma Qiang, Zhu Chuanda, Yang Yuanyuan, Lin Kerui, Li Yanglonghao, Zhang Qiang, Li Tiancheng, Lin Zhiqiang

Abstract excerpt

The approved small-molecule inhibitors of anaplastic lymphoma kinase (ALK) have shown remarkable efficacy in some subset of cancer patients. However, the numerous ALK mutants or fusion partners are resistant to such drugs, greatly limiting their application in clinic. Despite the drug design strategy of proteolysis-targeting chimera (PROTAC) holds great potential to overcome drug resistance in theory, there are...

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Identifiers

PMID: 37105002
DOI: 10.1016/j.bioorg.2023.106556

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Discovery of a miniaturized PROTAC with potent activity and high selectivity.PMID 37105002Read ↗

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