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Article

Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR.

Bioorganic & medicinal chemistry - 15 Jun 2015

Basu Debjit, Richters André, Rauh Daniel

Abstract excerpt

The clinical success of covalent kinase inhibitors in the treatment of EGFR-dependent non-small cell lung cancer (NSCLC) has rejuvenated the appreciation of reactive small molecules. Acquired drug resistance against first-line EGFR inhibitors remains the major bottleneck in NSCLC and is currently addressed by the application of fine-tuned covalent drugs. Here we report the design, synthesis and biochemical...

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Identifiers

PMID: 25975640
DOI: 10.1016/j.bmc.2015.04.038

Genes

EGFR

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