Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors
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https://figshare.com/articles/dataset/Discovery_of_Potent_Irreversible_Pan-Fibroblast_Growth_Factor_Receptor_FGFR_Inhibitors/5991079
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资源简介：
Fibroblast
growth factor receptors (FGFR1–4) are promising
therapeutic targets in many cancers. With the resurgence of interest
in irreversible inhibitors, efforts have been directed to the discovery
of irreversible FGFR inhibitors. Currently, several selective irreversible
inhibitors are being evaluated in clinical trials that could covalently
target a conserved cysteine in the P-loop of FGFR. In this article,
we used a structure-guided approach that is rationalized by a computer-aided
simulation to discover the novel and irreversible pan-FGFR inhibitor, 9g, which provided superior FGFR in vitro activities and decent
selectivity over VEGFR2 (vascular endothelia growth factor receptor
2). In in vivo studies, 9g displayed clear antitumor
activities in NCI-H1581 and SNU-16 xenograft mice models. Additionally,
the diluting method confirmed the irreversible binding of 9g to FGFR.
创建时间：
2018-03-15
