破解磷酸酶密码:对接相互作用决定底物特异性。
Cracking the phosphatase code: docking interactions determine substrate specificity.
机构信息
Department of Biology, Stanford University, 371 Serra Mall, Stanford, CA 94305-5020, USA.
出版信息
Sci Signal. 2009 Dec 8;2(100):re9. doi: 10.1126/scisignal.2100re9.
Phosphoserine- and phosphothreonine-directed phosphatases display remarkable substrate specificity, yet the sites that they dephosphorylate show little similarity in amino acid sequence. Studies reveal that docking interactions are key for the recognition of substrates and regulators by two conserved phosphatases, protein phosphatase 1 (PP1) and the Ca2+-calmodulin-dependent phosphatase calcineurin. In each case, a small degenerate sequence motif in the interacting protein directs low-affinity binding to a docking surface on the phosphatase that is distinct from the active site; several such interactions combine to confer overall binding specificity. Some docking surfaces are conserved, such as a hydrophobic groove on a face opposite the active site that serves as a major recognition surface for the "RVxF" motif of proteins that interact with PP1 and the "PxIxIT" motif of substrates of calcineurin. Secondary motifs combine with this primary targeting sequence to specify phosphatase binding. A comprehensive interactome for mammalian PP1 was described, analysis of which defines several PP1-binding motifs. Studies of "LxVP," a secondary calcineurin-binding sequence, establish that this motif is a conserved feature of calcineurin substrates and that the immunosuppressants FK506 and cyclosporin A inhibit the phosphatase by interfering with LxVP-mediated docking.
磷酸丝氨酸和磷酸苏氨酸定向磷酸酶表现出显著的底物特异性,但它们去磷酸化的位点在氨基酸序列上几乎没有相似性。研究表明,对接相互作用是两种保守的磷酸酶,即蛋白磷酸酶 1(PP1)和钙调蛋白依赖性磷酸酶钙调神经磷酸酶识别底物和调节剂的关键。在每种情况下,相互作用蛋白中的一个小简并序列基序指导低亲和力结合到磷酸酶上的对接表面,该表面与活性位点不同;几个这样的相互作用结合起来赋予整体结合特异性。一些对接表面是保守的,例如与活性位点相对的面上的疏水性凹槽,它是与 PP1 相互作用的“RVxF”基序的蛋白质和钙调神经磷酸酶的底物的“PxIxIT”基序的主要识别表面。次要基序与这个主要靶向序列结合指定磷酸酶结合。描述了哺乳动物 PP1 的综合相互作用组,对其的分析定义了几个 PP1 结合基序。对“LxVP”(一种次要钙调神经磷酸酶结合序列)的研究确立了该基序是钙调神经磷酸酶底物的保守特征,免疫抑制剂 FK506 和环孢菌素 A 通过干扰 LxVP 介导的对接来抑制磷酸酶。