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7次跨膜受体二聚化的功能后果。

Functional consequences of 7TM receptor dimerization.

作者信息

Hansen Jakob Lerche, Sheikh Søren P

机构信息

Laboratory of Molecular Cardiology, The Heart Centre and Copenhagen Heart Arrhythmia Research Centre (CHARC), Copenhagen University Hospital, Faculty of Health, University of Copenhagen, 20 Juliane Mariesvej, Denmark.

出版信息

Eur J Pharm Sci. 2004 Dec;23(4-5):301-17. doi: 10.1016/j.ejps.2004.08.004.

Abstract

7TM receptors work as signaling platforms that activate multiple signalling systems at the intracellular face of the plasma membrane. It is an emerging concept that 7TM receptors form homo- and hetero-dimers or -oligomers in vitro and in vivo. Numerous studies suggest dimerization is important for receptor function including agonist/antagonist affinity, efficacy, trafficking, and specificity of signal transduction, yet it remains unknown whether dimerization is a prerequisite for 7TM receptor signaling. The current review provides an overview of the biochemical support for 7TM homodimerization, followed by a discussion of the characteristics of homodimerization, with focus on dimer organization, and the functional consequences of dimerization. Heterodimerization will not generally be discussed in this review although we have included a few examples to illustrate specific points, and a table that summarises the current literature on this subject.

摘要

7次跨膜受体作为信号平台,在质膜的细胞内表面激活多个信号系统。7次跨膜受体在体外和体内形成同二聚体、异二聚体或寡聚体,这是一个正在兴起的概念。大量研究表明,二聚化对于受体功能很重要,包括激动剂/拮抗剂亲和力、效力、转运和信号转导特异性,但二聚化是否是7次跨膜受体信号传导的先决条件仍不清楚。本综述概述了7次跨膜同二聚化的生化支持,随后讨论了同二聚化的特征,重点是二聚体结构以及二聚化的功能后果。尽管我们列举了一些例子来说明特定要点,并给出了一个总结该主题当前文献的表格,但本综述一般不会讨论异二聚化。

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