[1]刘 磊,许婵娟,刘剑峰.GABAB受体变构调节剂及其应用研究进展[J].中国药理学通报,2018,(10):1352-1355.[doi:10.3969/j.issn.1001-1978.2018.10.006]
 LIU Lei,XU Chan-juan,LIU Jian-feng.Research progress of GABAB receptor allosteric modulators and their applications[J].Chinese Pharmacological Bulletin,2018,(10):1352-1355.[doi:10.3969/j.issn.1001-1978.2018.10.006]
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GABAB受体变构调节剂及其应用研究进展()
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《中国药理学通报》[ISSN:/CN:]

卷:
期数:
2018年10期
页码:
1352-1355
栏目:
讲座与综述
出版日期:
2018-09-26

文章信息/Info

Title:
Research progress of GABAB receptor allosteric modulators and their applications
文章编号:
1001-1978(2018)10-1352-04
作者:
刘 磊 许婵娟 刘剑峰
华中科技大学生命科学与技术学院,湖北 武汉 430074
Author(s):
LIU Lei XU Chan-juan LIU Jian-feng
College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan 430074, China
关键词:
GABAB受体 正位位点 正位配体 变构调节位点 变构调节剂 动物模型
Keywords:
GABAB receptor orthosteric site orthosteric ligand allosteric site allosteric modulator animal model
分类号:
R-05; R392.11
DOI:
10.3969/j.issn.1001-1978.2018.10.006
文献标志码:
A
摘要:
GABAB受体参与调控多种重要生理和病理过程,是重要药物靶点之一。目前,针对该受体的药物开发主要为其正位配体,上市药物非常有限。变构调节剂是GABAB受体的新型配体,通过作用于GABAB受体变构调节位点,特异性调控受体活性,具有很好的受体特异性和药理学特性。多种动物模型实验结果显示,GABAB受体变构调节剂可以协同正位配体,有效改善如药物成瘾、疼痛等多种疾病症状,并具有不同于正位配体的药效特点。GABAB受体变构调节剂生理效应机制较独特,具有较好的医药应用价值和前景,进一步的临床试验验证和变构调节剂精细作用机制的深入研究,将为新药开发提供新思路。该文介绍了GABAB受体变构调节剂的最新研究及其应用进展,并对这类化合物的作用优势和应用前景进行概述。
Abstract:
GABAB receptor involves in the regulation of diverse physiological and pathological processes and has been one of the most important drug targets.Currently, drug development for the receptor mainly focuses on orthosteric ligands, and the marketed drugs are very limited.Allosteric modulators are novel ligands of the GABAB receptor, which specifically regulate receptor activity by acting on the allosteric modulatory sites and possess good receptor specificity and pharmacological characteristics.A variety of animal model experiments showed that GABAB receptor allosteric modulators could effectively improve the symptoms of various diseases, such as drug addiction and pain, by cooperating with orthosteric ligands, and exert novel characteristics other than orthosteric ligands.The unique physiological effects of GABAB receptor allosteric modulators set them as promising candidates, showing excellent medical application value and prospects.Further clinical trial verification and investigation of the detailed mechanism of allosteric modulators will provide new ideas for the development of new drugs.

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备注/Memo

备注/Memo:
收稿日期:2015-05-25,修回日期:2018-07-20
基金项目:国家自然科学基金资助项目(No 31711530146,31511130131,31301163)
作者简介:刘 磊(1986-),男,博士生,研究方向:GABAB受体变构调节,E-mail:lei_liu86@163.com;
刘剑峰(1971-),男,博士,教授,博士生导师,研究方向:C族GPCRs结构与功能,通讯作者,E-mail:jfliu@hust.edu.cn
更新日期/Last Update: 2018-08-26