基诺美
表皮生长因子受体
化学
癌症研究
激酶
脊索瘤
内科学
生物
生物化学
受体
医学
病理
作者
Christopher R. M. Asquith,Kaleb M. Naegeli,Michael P. East,Tuomo Laitinen,Tammy M. Havener,Carrow I. Wells,Gary L. Johnson,David H. Drewry,William J. Zuercher,David C. Morris
标识
DOI:10.1021/acs.jmedchem.9b00350
摘要
We describe the design of a set of inhibitors to investigate the relationship between cyclin G associated kinase (GAK) and epidermal growth factor receptor (EGFR) in chordoma bone cancers. These compounds were characterized both in vitro and using in cell target engagement assays. The most potent chordoma inhibitors were further characterized in a kinome-wide screen demonstrating narrow spectrum profiles. While we observed a direct correlation between EGFR and antiproliferative effects on chordoma, GAK inhibition appeared to have only a limited effect.
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