THEMED ISSUE: GPCR REVIEW G protein-coupled receptor hetero-dimerization: contribution to pharmacology and function
THEMED ISSUE: GPCR REVIEW G protein-coupled receptor hetero-dimerization: contribution to pharmacology and function
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发表时间：
2009
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通讯作者：
G. Milligan
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作者：
G. Milligan
G蛋白偶联受体（GPCR）可以形成异源二聚体或异源寡聚体的概念继续获得实验支持。然而，除了 GABAB 受体以及甜味和鲜味受体外，很少有报道的例子符合最近国际基础和临床药理学联合会赞助的审查（Pin 等人，2007 年）中建议的所有标准，这些标准应该被要求定义不同的和生理相关的受体种类。尽管如此，仍有许多例子表明成对的共表达 GPCR 相互调节其功能、运输和/或配体药理学。这些数据至少与受体对之间的物理相互作用一致。近年来，有人提出，特定的 GPCR 异二聚体或异寡聚体对可能代表某些临床有效的小分子药物的关键分子靶标，并且人们越来越关注鉴定可选择性调节异二聚体功能的配体。当前的评论总结了这些主题的最新主要进展。英国药理学杂志 (2009) 158, 5–14; doi:10.1111/j.1476-5381.2009.00169.x； 2009 年 3 月 20 日在线发布
The concept that G protein-coupled receptors (GPCRs) can form hetero-dimers or hetero-oligomers continues to gain experimental support. However, with the exception of the GABAB receptor and the sweet and umami taste receptors few reported examples meet all of the criteria suggested in a recent International Union of Basic and Clinical Pharmacology sponsored review (Pin et al., 2007) that should be required to define distinct and physiologically relevant receptor species. Despite this, there are many examples in which pairs of co-expressed GPCRs reciprocally modulate their function, trafficking and/or ligand pharmacology. Such data are at least consistent with physical interactions between the receptor pairs. In recent times, it has been suggested that specific GPCR hetero-dimer or hetero-oligomer pairs may represent key molecular targets of certain clinically effective, small molecule drugs and there is growing interest in efforts to identify ligands that may modulate hetero-dimer function selectively. The current review summarizes key recent developments in these topics. British Journal of Pharmacology (2009) 158, 5–14; doi:10.1111/j.1476-5381.2009.00169.x; published online 20 March 2009