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G蛋白偶联受体变构调节作用的研究进展 被引量：1

Allosteric regulation of G-protein coupled receptors
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摘要 G蛋白偶联受体(GPCRs)是极为重要的药物靶点,提高靶向GPCRs药物的选择性和高效性仍是新药研发必须面对的关键性问题。GPCRs变构调节的研究结果表明,其变构作用机制和调节位点存在着复杂的多样性。GPCRs变构调节作用的研究可能会为受体亚型高选择性和高效性新药的研究提供新的契机。该文总结、归纳了近年来GPCRs变构调节作用的研究进展,以便较全面地了解GPCRs变构调节机制及其生物学意义。 Despite the important properties of GPCRs as drug targets, improving the subtype selectivity and efficiency of new drugs targeting at GPCRs is a predominant challenge. The study of GPCRs allosterism shows there exist great complexity and diversity in allosterism and allosteric sites, and it also provides a new opportunity for exploring new drugs with subtype selectivity and efficiency. This review summaries the development of GPCRs allosterism in recent years and shows GPCRs allosterism and its biological significance.
作者 牟男 王丽韫 郑建全
机构地区 军事医学科学院毒物药物研究所
出处 《中国药理学通报》 CAS CSCD 北大核心 2008年第7期853-857,共5页 Chinese Pharmacological Bulletin
基金 国家自然科学基金面上资助项目(No203900508)
关键词 G蛋白偶联受体 变构调节 GPCRs allosteric regulation
分类号 R-05 [医药卫生] R341.3 [医药卫生—基础医学]
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参考文献27

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中国药理学通报
2008年 第7期

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