Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer
作者： Lingfeng Chen , Weitao Fu , Lulu Zheng , Zhiguo Liu , Guang Liang
DOI: 10.1021/ACS.JMEDCHEM.7B01310
关键词:
摘要: The epidermal growth factor receptor (EGFR) has been a particular interest for drug development treatment of non-small-cell lung cancer (NSCLC). current third-generation EGFR small-molecule inhibitors, especially osimertinib, are at the forefront clinically patients with NSCLC. However, high percentage these treated developed tertiary cystein-797 to serine-790 (C797S) mutation in kinase domain. This C797S is thought induce resistance all irreversible TKIs. In this Miniperspective, we present key mechanisms response TKIs, and emerging reports on novel TKIs combat resistance. Specifically, analyze allosteric ATP-competitive inhibitors terms discovery, binding mechanism, their potency selectivity against harboring mutations. Lastly, provide some perspectives new challenges future directions field.
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