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Validation of ion mobility spectrometry - mass spectrometry as a screening tool to identify type II kinase inhibitors of FGFR1 kinase
Rapid Communications in Mass Spectrometry ( IF 1.8 ) Pub Date : 2021-05-26 , DOI: 10.1002/rcm.9130
Helen S Beeston 1 , Tobias Klein 2 , Richard A Norman 2 , Julie A Tucker 2 , Malcolm Anderson 2 , Alison E Ashcroft 1 , Geoffrey A Holdgate 2
Affiliation  

The protein kinase FGFR1 regulates cellular processes in human development. As over-activity of FGFR1 is implicated with cancer, effective inhibitors are in demand. Type I inhibitors, which bind to the active form of FGFR1, are less effective than type II inhibitors, which bind to the inactive form. Screening to distinguish between type I and type II inhibitors is required.

中文翻译:


验证离子迁移谱-质谱法作为鉴定 FGFR1 激酶 II 型激酶抑制剂的筛选工具



蛋白激酶 FGFR1 调节人类发育中的细胞过程。由于 FGFR1 的过度活性与癌症有关,因此需要有效的抑制剂。 I 型抑制剂与 FGFR1 的活性形式结合,其效果不如与非活性形式结合的 II 型抑制剂。需要进行筛选以区分 I 型和 II 型抑制剂。
更新日期:2021-05-26
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