Allosteric interactions among drug binding sites on calmodulin.
Allosteric interactions among drug binding sites on calmodulin.
复制标题
钙调蛋白上药物结合位点之间的变构相互作用。
DOI：
10.1016/0006-291x(83)91530-9
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发表时间：
1983
影响因子：
3.1
通讯作者：
J. Johnson
中科院分区：
文献类型：
--
作者：
J. Johnson
非洛地平是一种荧光二氢吡啶类钙拮抗剂。它以Ca2+依赖的方式与钙调蛋白结合，并经历荧光增加，这使我们能够监测其与钙调蛋白的相互作用。包括钙调蛋白拮抗剂R24571和Ca2+拮抗剂异戊二烯胺和地尔硫卓在内的疏水配体与钙调蛋白结合，并使非洛地平结合增强多达20倍。这些研究表明，钙调素上不同的药物结合位点之间发生变构相互作用。我们的结果进行了讨论的钙调素的作用机制。
Felodipine is a fluorescent dihydropyridine Ca2+-antagonist. It binds to calmodulin in a Ca2+-dependent manner, and undergoes a fluorescence increase which allows us to monitor its interaction with calmodulin. Hydrophobic ligands including the calmodulin antagonist, R24571 and Ca2+antagonists, prenylamine and diltiazem, bind to calmodulin and potentiate felodipine binding by as much as 20 fold. These studies suggest that allosteric interactions occur among different drug binding sites on calmodulin. Our results are discussed in terms of the mechanism of action of calmodulin.