Ontology highlight
ABSTRACT:
SUBMITTER: Cheng M
PROVIDER: S-EPMC7318554 | biostudies-literature | 2020 Feb
REPOSITORIES: biostudies-literature
Cheng Meng M Yu Xufen X Lu Kaylene K Xie Ling L Wang Li L Meng Fanye F Han Xiaoran X Chen Xian X Liu Jing J Xiong Yue Y Jin Jian J
Journal of medicinal chemistry 20200114 3
Several epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors have been developed and approved by Food and Drug Administration for the treatment of non-small-cell lung cancers, but their efficacy can be compromised by acquired drug resistance conferred by <i>EGFR</i>-mutant variants. Here, we described the discovery of a novel E3 ligase von Hippel-Lindau-recruiting EGFR degrader, MS39 (compound <b>6</b>), and a first-in-class E3 ligase cereblon-recruiting EGFR degrader, MS154 (compo ...[more]