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顺式尿刊酸作为5-羟色胺（2A）受体激动剂的分子基础。

Molecular basis for cis-urocanic acid as a 5-HT(2A) receptor agonist.

作者信息

Shen Liang, Ji Hong-Fang

机构信息

Shandong Provincial Research Center for Bioinformatic Engineering and Technique, Center for Advanced Study, Shandong University of Technology, Zibo 255049, PR China.

出版信息

Bioorg Med Chem Lett. 2009 Sep 15;19(18):5307-9. doi: 10.1016/j.bmcl.2009.07.143. Epub 2009 Aug 3.

DOI:10.1016/j.bmcl.2009.07.143
PMID:19683920
Abstract

The underlying mechanisms of urocanic acid (UA) to induce immune suppression remain elusive until the recent finding that cis-UA acts via the serotonin, 5-hydroxytryptamine (5-HT) receptor subtype 5-HT(2A). In the present study, the interactions of cis-UA to 5-HT(2A) receptor were explored and compared with those of 5-HT to the same receptor using computational docking. Similar binding modes were observed for cis-UA and 5-HT with 5-HT(2A) receptor and the former possessed relatively higher binding affinity, which may account for cis-UA being a serotonin receptor agonist. Moreover, the molecular basis for the distinct binding affinities between the trans- and cis-UA with 5-HT(2A) receptor was also provided.

摘要

尿刊酸（UA）诱导免疫抑制的潜在机制一直不明，直到最近发现顺式-UA通过血清素、5-羟色胺（5-HT）受体亚型5-HT(2A)发挥作用。在本研究中，利用计算对接技术探索了顺式-UA与5-HT(2A)受体的相互作用，并将其与5-HT与同一受体的相互作用进行了比较。观察到顺式-UA和5-HT与5-HT(2A)受体具有相似的结合模式，且前者具有相对较高的结合亲和力，这可能解释了顺式-UA是一种血清素受体激动剂。此外，还提供了反式-UA和顺式-UA与5-HT(2A)受体之间不同结合亲和力的分子基础。

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