EGF 受体中的催化控制及其与一般激酶调节机制的联系。
Catalytic control in the EGF receptor and its connection to general kinase regulatory mechanisms.
机构信息
Department of Molecular and Cell Biology, University of California, Berkeley, Berkeley, CA 94720, USA.
出版信息
Mol Cell. 2011 Apr 8;42(1):9-22. doi: 10.1016/j.molcel.2011.03.004.
Abstract
In contrast to the active conformations of protein kinases, which are essentially the same for all kinases, inactive kinase conformations are structurally diverse. Some inactive conformations are, however, observed repeatedly in different kinases, perhaps reflecting an important role in catalysis. In this review, we analyze one of these recurring conformations, first identified in CDK and Src kinases, which turned out to be central to understanding of how kinase domain of the EGF receptor is activated. This mechanism, which involves the stabilization of the active conformation of an α helix, has features in common with mechanisms operative in several other kinases.
摘要
与所有激酶基本相同的蛋白激酶的活性构象相反，无活性激酶构象在结构上是多种多样的。然而，一些无活性构象在不同的激酶中反复出现，这也许反映了它们在催化中的重要作用。在这篇综述中，我们分析了其中一种反复出现的构象，这种构象最初在 CDK 和Src 激酶中被发现，后来被证明对于理解 EGF 受体激酶结构域的激活机制至关重要。这个机制涉及到一个α螺旋的活性构象的稳定，它与几个其他激酶中的作用机制有共同之处。
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