Article
Identification of novel drug-resistant EGFR mutant inhibitors by in silico screening using comprehensive assessments of protein structures.
Bioorganic & medicinal chemistry - 15 Jun 2012
Sato Tomohiro, Watanabe Hisami, Tsuganezawa Keiko, Yuki Hitomi, Mikuni Junko, Yoshikawa Seiko, Kukimoto-Niino Mutsuko, Fujimoto Takako, Terazawa Yumiko, Wakiyama Motoaki, Kojima Hirotatsu, Okabe Takayoshi, Nagano Tetsuo, Shirouzu Mikako, Yokoyama Shigeyuki, Tanaka Akiko, Honma Teruki
Abstract excerpt
EGFR is a target protein for the treatment of non small cell lung cancer (NSCLC). The mutations associated with the activation of EGFR kinase activity, such as L858R and G719S, destabilize the inactive conformation of EGFR and are closely linked with the development of NSCLC. The additional T790M mutation reportedly causes drug resistance against the commercially available EGFR inhibitors, gefitinib and...
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