Article
Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase.
PloS one - 1 Jan 2015
Moccia Marialuisa, Liu Qingsong, Guida Teresa, Federico Giorgia, Brescia Annalisa, Zhao Zheng, Choi Hwan Geun, Deng Xianming, Tan Li, Wang Jinhua, Billaud Marc, Gray Nathanael S, Carlomagno Francesca, Santoro Massimo
Abstract excerpt
Oncogenic mutation of the RET receptor tyrosine kinase is observed in several human malignancies. Here, we describe three novel type II RET tyrosine kinase inhibitors (TKI), ALW-II-41-27, XMD15-44 and HG-6-63-01, that inhibit the cellular activity of oncogenic RET mutants at two digit nanomolar concentration. These three compounds shared a 3-trifluoromethyl-4-methylpiperazinephenyl pharmacophore that stabilizes...
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