ATP 竞争型激酶抑制剂对蛋白质相互作用的潜伏变构调控。
Latent allosteric control of protein interactions by ATP-competitive kinase inhibitors.
机构信息
Department of Biochemistry, University of Colorado Boulder, Boulder CO 80303, USA.
Department of Biochemistry, University of Colorado Boulder, Boulder CO 80303, USA.
出版信息
Curr Opin Struct Biol. 2024 Dec;89:102935. doi: 10.1016/j.sbi.2024.102935. Epub 2024 Oct 11.
Abstract
Protein kinase inhibitors designed to compete with ATP as a primary mode of action turn out to have considerable effects that go beyond their interference of nucleotide binding. New research shows how kinase activation and sometimes noncatalytic functions of protein kinases can be controlled by allosteric properties of kinase inhibitors, communicating perturbations from the active site to distal regulatory regions.
摘要
蛋白激酶抑制剂的设计初衷是作为主要作用模式与 ATP 竞争，结果发现它们具有超出核苷酸结合干扰的相当大的作用。新的研究表明，激酶抑制剂的别构特性如何控制激酶的激活和有时非催化功能，将来自活性位点的扰动传递到远端调节区域。
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