LY2874455 potently inhibits FGFR gatekeeper mutants and overcomes mutation-based resistance

Daichao Wu; Ming Guo; Xiaoli Min; Shuyan Dai; Meixiang Li; Sijie Tan; Guoqing Li; Xiaojuan Chen; Yao Ma; Jun Li; Longying Jiang; Lingzhi Qu; Zhan Zhou; Zhuchu Chen; Lin Chen; Guangyu Xu; Yongheng Chen

doi:10.1039/C8CC07546H

LY2874455 potently inhibits FGFR gatekeeper mutants and overcomes mutation-based resistance†

Daichao Wu,^ab Ming Guo,^a Xiaoli Min,^a Shuyan Dai,^a Meixiang Li,^b Sijie Tan,^b Guoqing Li,^b Xiaojuan Chen,^a Yao Ma,^c Jun Li,^a Longying Jiang,^a Lingzhi Qu,^a Zhan Zhou,^a Zhuchu Chen,^a Lin Chen,^d Guangyu Xu^e and Yongheng Chen*^a

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* Corresponding authors

^a Laboratory of Structural Biology, Key Laboratory of Cancer Proteomics of Chinese Ministry of Health, XiangYa Hospital, Central South University, Changsha, Hunan 410008, China
E-mail: yonghenc@163.com

^b Department of Histology and Embryology, Institute of Clinical Anatomy & Reproductive Medicine, Medical College, University of South China, Hengyang, Hunan 421001, China

^c Network Information Center, University of South China, Hengyang, Hunan 421001, China

^d Molecular and Computational Biology, Department of Biological Sciences, University of Southern California, Los Angeles, CA 90089, USA

^e Key Laboratory of Chemical Biology and Traditional Chinese Medicine Research (Ministry of Education), College of Chemistry and Chemical Engineering, Hunan Normal University, Changsha 410081, China

Abstract

The chemical compound LY2874455 has the potential to overcome drug resistance driven by FGFR gatekeeper mutations. X-ray crystallographic studies provide the structural explanation for why this compound is effective against the FGFR gatekeeper mutations.

Chemical Communications

LY2874455 potently inhibits FGFR gatekeeper mutants and overcomes mutation-based resistance†

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LY2874455 potently inhibits FGFR gatekeeper mutants and overcomes mutation-based resistance

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