II 型和 III 型代谢型谷氨酸受体药物化学的最新进展。
Recent advances in the medicinal chemistry of group II and group III mGlu receptors.
作者信息
Jin Chaobin, Ma Shutao
机构信息
Department of Medicinal Chemistry , Key Laboratory of Chemical Biology (Ministry of Education) , School of Pharmaceutical Sciences , Shandong University , 44, West Culture Road , Jinan 250012 , P.R. China . Email:
出版信息
Medchemcomm. 2017 Jan 13;8(3):501-515. doi: 10.1039/c6md00612d. eCollection 2017 Mar 1.
Abstract
Metabotropic glutamate receptors (mGlu receptors) belong to the G-protein-coupled receptors superfamily. They are divided into three groups, in which group II and group III belong to presynaptic receptors that negatively modulate glutamate and γ-aminobutyric acid (GABA) release when activated. In this review, we introduce not only the functions of mGlu receptors, but also the group II and group III allosteric modulators and agonists/antagonists reported over the past five years according to a classification of their structures, with a specific focus on their biological activity and selectivity. In particular, the structure of these compounds and the future directions of ideal candidates are highlighted.
摘要
代谢型谷氨酸受体（mGlu受体）属于G蛋白偶联受体超家族。它们分为三组，其中第二组和第三组属于突触前受体，激活时可负向调节谷氨酸和γ-氨基丁酸（GABA）的释放。在本综述中，我们不仅介绍了mGlu受体的功能，还根据其结构分类介绍了过去五年报道的第二组和第三组变构调节剂以及激动剂/拮抗剂，特别关注它们的生物活性和选择性。尤其突出了这些化合物的结构以及理想候选物的未来发展方向。
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