Journal of medicinal chemistryHumansDrug DesignDrug ResistanceNeoplasmAnimals
Design, Synthesis, and Biological Evaluation of the First Novel Macrocycle-Based FGFR Inhibitors That Overcome Clinically Acquired Resistance.
Shuang Xiang, Xiaojuan Chen, Jieying Lin, Xiaojing Lin, Qianmeng Lin, Xiaojuan Song, Ling Yan, Haoran Peng, Zhengchao Tu, Adam V Patterson, Jeff B Smaill, Yalin Tu, Yongheng Chen, Xiaoyun Lu
Published: 202610.1021/acs.jmedchem.5c02462
Abstract
Alterations in the FGFR family act as oncogenic drivers for multiple pediatric and adult tumors, leading to the development and approval of several FGFR inhibitors. However, the on-target gatekeeper and "molecular brake" mutations confer clinically a…
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