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G-protein coupled receptor oligomerization in neuroendocrine pathways
Frontiers in Neuroendocrinology ( IF 6.5 ) Pub Date : 2003-12-01 , DOI: 10.1016/j.yfrne.2003.10.002
Karen M Kroeger 1 , Kevin D G Pfleger , Karin A Eidne
Affiliation  

Protein-protein interactions are fundamental processes for many biological systems including those involving the superfamily of G-protein coupled receptors (GPCRs). A growing body of biochemical and functional evidence supports the existence of GPCR-GPCR homo- and hetero-oligomers. In particular, hetero-oligomers can display pharmacological and functional properties distinct from those of the homodimer or oligomer thus adding another level of complexity to how GPCRs are activated, signal and traffick in the cell. Dimerization may also play a role in influencing the activity of agonists and antagonists. We are only beginning to unravel how and why such complexes are formed, the functional implications of which will have an enormous impact on GPCR biology. Future research that studies GPCRs as dimeric or oligomeric complexes will enhance not only our understanding of GPCRs in cellular function but will also be critical for novel drug design and improved treatment of the vast array of GPCR-related conditions.

中文翻译:

神经内分泌通路中的 G 蛋白偶联受体寡聚化

蛋白质-蛋白质相互作用是许多生物系统的基本过程,包括那些涉及 G 蛋白偶联受体 (GPCR) 超家族的系统。越来越多的生化和功能证据支持 GPCR-GPCR 同源和异源寡聚体的存在。特别是,异源寡聚体可以显示出不同于同源二聚体或寡聚体的药理学和功能特性,从而为 GPCR 在细胞中的激活、信号和运输方式增加了另一层次的复杂性。二聚化也可能在影响激动剂和拮抗剂的活性方面发挥作用。我们才刚刚开始阐明这种复合物是如何以及为何形成的,其功能意义将对 GPCR 生物学产生巨大影响。
更新日期:2003-12-01
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