Compound Selectivity and Target Residence Time of Kinase Inhibitors Studied with Surface Plasmon Resonance

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• 作者：Nicole Willemsen-Seegers¹ ; Joost C.M. Uitdehaag¹ ; Martine B.W. Prinsen¹ ; Judith R.F. de Vetter¹ ; Jos de Man¹ ; Masaaki Sawa² ; Yusuke Kawase² ; Rogier C. Buijsman¹ ; Guido J.R. Zaman¹ ; ^{guido.zaman@ntrc.nl}
• 关键词：FDA ; US Food and Drug Administration ; EGFR ; epidermal growth factor receptor ; BTK ; Bruton's tyrosine kinase ; SPR ; surface plasmon resonance ; PI3K ; phosphoinositide 3-kinase ; SD ; standard deviation ; SE ; standard error ; PI3K ; phosphoinositide 3-kinase ; SPR ; surface plasmon resonance
• 刊名：Journal of Molecular Biology
• 出版年：2017
• 出版时间：17 February 2017
• 年：2017
• 卷：429
• 期：4
• 页码：574-586
• 全文大小：801 K
• 卷排序：429

文摘

Resource of on- and off-rates of important kinase inhibitor drug interactions Analysis of the binding of irreversible tyrosine kinase inhibitors in real time Known “pan”-Aurora kinase inhibitors reside longer on Aurora B than Aurora A. Idelalisib and duvelisib have same selectivity for δ- over γ-isoform PI3K.