钙结合蛋白 D28k 和 S100B 与具有相似相互作用位点的锂抑制性酶肌醇单磷酸酶-1：一个新的药物靶点。

Calbindin D28k and S100B have a similar interaction site with the lithium-inhibitable enzyme inositol monophosphatase-1: a new drug target site.

机构信息

Department of Clinical Biochemistry and Pharmacology, Faculty of Health Sciences, and ‡Mental Health Center, Ben-Gurion University of the Negev , Beer-Sheva 84105, Israel.

出版信息

J Med Chem. 2015 Feb 26;58(4):2042-4. doi: 10.1021/jm5019324. Epub 2015 Feb 16.

DOI:10.1021/jm5019324

Abstract

Lithium salts (Li) are used to treat bipolar disorder patients. Li inhibits inositol-monophosphatase (IMPase)-1. Calbindin D28k (calbindin) and S100B enhance IMPase-1 activity. We compared our in silico model of the IMPase-1/calbindin complex with the crystal structure of S100B. Although calbindin and S100B have a low sequence homology, they seem to activate IMPase-1 in a similar mode. It is reasonable that molecules interfering with the interaction of IMPase-1 with either of its activators will have Li-like effects.

摘要

锂盐（Li）用于治疗双相情感障碍患者。Li 抑制肌醇单磷酸酶（IMPase）-1。钙结合蛋白 D28k（钙结合蛋白）和 S100B 增强 IMPase-1 活性。我们比较了肌醇单磷酸酶-1/钙结合蛋白复合物的计算机模型与 S100B 的晶体结构。尽管钙结合蛋白和 S100B 的序列同源性较低，但它们似乎以相似的方式激活 IMPase-1。合理的是，干扰 IMPase-1 与其任一激活剂相互作用的分子将具有类似 Li 的作用。

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