Quantitative, wide-spectrum kinase profiling in live cells for assessing the effect of cellular ATP on target engagement

For kinase inhibitors, intracellular target selectivity is fundamental to pharmacological mechanism. Although a number of acellular techniques have been developed to measure kinase binding or enzymatic inhibition, such approaches can fail to accurately predict engagement in cells. Here we report the...

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Main Authors: Vasta, JD, Corona, CR, Wilkinson, J, Zimprich, CA, Hartnett, JR, Ingold, MR, Zimmerman, K, Machleidt, T, Kirkland, TA, Huwiler, KG, Ohana, RF, Slater, M, Otto, P, Cong, M, Wells, CI, Berger, B-T, Hanke, T, Glas, C, Ding, K, Drewry, DH, Huber, KVM, Willson, TM, Knapp, S, Müller, S, Meisenheimer, PL, Fan, F, Wood, KV, Robers, MB
格式: Journal article
語言:English
出版: Cell Press 2017