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通过SIE方法对多巴胺D2受体拮抗剂结合情况的预测。

Predictions of binding for dopamine D2 receptor antagonists by the SIE method.

作者信息

Wang Yeng-Tseng, Su Zhi-Yuan, Hsieh Chang-Huain, Chen Cheng-Lung

机构信息

National Center for High-performance Computing, Hsin-Shi, Tainan County 741, Taiwan.

出版信息

J Chem Inf Model. 2009 Oct;49(10):2369-75. doi: 10.1021/ci9002238.

Abstract

The control of tetralindiol derivative antagonists released through the inhibition of dopamine D2 receptors has been identified as a potential target for the treatment of schizophrenia. We employed molecular dynamics simulation techniques to identify the predicted D2 receptor structure. Homology models of the protein were developed on the basis of crystal structures of four receptor crystals. Compound docking revealed the possible binding mode. In addition, the docking analyses results indicate that five residues (Asp72, Val73, Cys76, Leu183, and Phe187) were responsible for the selectivity of the tetralindiol derivatives. Our molecular dynamics simulations were applied in combination with the solvated interaction energies (SIE) technique to predict the compounds' docking modes in the binding pocket of the D2 receptor. The simulations revealed satisfactory correlations between the calculated and experimental binding affinities of all seven tetralindiol derivative antagonists, as indicated by the obtained R2 value of 0.815.

摘要

通过抑制多巴胺D2受体释放来控制四氢萘二醇衍生物拮抗剂已被确定为治疗精神分裂症的一个潜在靶点。我们采用分子动力学模拟技术来确定预测的D2受体结构。基于四种受体晶体的晶体结构构建了该蛋白质的同源模型。化合物对接揭示了可能的结合模式。此外,对接分析结果表明,五个残基(Asp72、Val73、Cys76、Leu183和Phe187)负责四氢萘二醇衍生物的选择性。我们将分子动力学模拟与溶剂化相互作用能(SIE)技术相结合,以预测化合物在D2受体结合口袋中的对接模式。模拟结果显示,所有七种四氢萘二醇衍生物拮抗剂的计算结合亲和力与实验结合亲和力之间具有令人满意的相关性,所得R2值为0.815即表明了这一点。

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