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Article

Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands.

Journal of medicinal chemistry - 24 Mar 2022

Zhao Hong-Yi, Wang Hai-Peng, Mao Yu-Ze, Zhang Hao, Xin Minhang, Xi Xiao-Xiao, Lei Hao, Mao Shuai, Li Dong-Hui, Zhang San-Qi

Abstract excerpt

Drug resistance caused by epidermal growth factor receptor (EGFR) mutation has largely limited the clinical use of EGFR tyrosine kinase inhibitors (EGFR-TKIs) for the treatment of non-small-cell lung cancer (NSCLC). Herein, to overcome the intractable problem of drug resistance, proteolysis targeting chimeras (PROTACs) targeting EGFR mutants were developed by optimizing covalent EGFR ligands. Covalent or...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 35254067
DOI: 10.1021/acs.jmedchem.1c01827

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026.

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Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands.PMID 35254067Read ↗

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Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting C797S Mutation.Semantic proximity Read ↗

Cetuximab-based PROteolysis targeting chimera for effectual downregulation of NSCLC with varied EGFR mutations.Semantic proximity Read ↗

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