Pin Jean-Philippe, Neubig Richard, Bouvier Michel, Devi Lakshmi, Filizola Marta, Javitch Jonathan A, Lohse Martin J, Milligan Graeme, Palczewski Krzysztof, Parmentier Marc, Spedding Michael
Institut de Génomique Fonctionnelle, 141, rue de la Cardonille, 34094 Montpellier cedex 5, France.
Pharmacol Rev. 2007 Mar;59(1):5-13. doi: 10.1124/pr.59.1.5.
G protein-coupled receptors (GPCRs) have long been considered to be monomeric membrane proteins. Although numerous recent studies have indicated that GPCRs can form multimeric complexes, the functional and pharmacological consequences of this phenomenon have remained elusive. With the discovery that the functional GABA(B) receptor is an obligate heterodimer and with the use of energy transfer technologies, it is now accepted that GPCRs can form heteromultimers. In some cases, specific properties of such heteromers not shared by their respective homomers have been reported. Although in most cases these properties have only been observed in heterologous expression systems, there are a few reports describing data consistent with such heteromultimeric GPCR complexes also existing in native tissues. The present article illustrates well-documented examples of such native multimeric complexes, lists a number of recommendations for recognition and acceptance of such multimeric receptors, and gives recommendations for their nomenclature.
G蛋白偶联受体(GPCRs)长期以来一直被认为是单体膜蛋白。尽管最近大量研究表明GPCRs能形成多聚体复合物,但这一现象的功能和药理学后果仍不清楚。随着功能性γ-氨基丁酸B型(GABA(B))受体被发现是一种 obligate 异二聚体以及能量转移技术的应用,现在人们已经接受GPCRs能形成异源多聚体。在某些情况下,已经报道了这些异源多聚体具有一些其各自同源多聚体所没有的特定特性。尽管在大多数情况下这些特性仅在异源表达系统中被观察到,但有一些报道描述的数据与天然组织中也存在这种异源多聚体GPCR复合物一致。本文阐述了这类天然多聚体复合物的充分记录的例子,列出了一些关于识别和接受这类多聚体受体的建议,并给出了它们的命名建议。