Satake Honoo, Sakai Tsubasa
Suntory Institute for Bioorganic Research, Wakayamadai 1-1-1, Shimamoto-cho, Mishima-gun, Osaka 618-8503, Japan.
Protein Pept Lett. 2008;15(3):300-8. doi: 10.2174/092986608783744207.
G protein coupled-receptors (GPCR) have been shown to form heterodimers or heterooligomers with various biochemical and/or pharmacological activity that are distinct from those of the corresponding monomers or homomers. Recent in vitro and in vivo experimental data have also shown novel functional roles of several orphan GPCRs as modulatory units of heterodimers and potentials for development of heterodimer-selective clinical agents. In this review, we summarize essential and latest knowledge as to GPCR heterodimerizations and the current issues to be solved in the near future.
G蛋白偶联受体（GPCR）已被证明能与各种具有不同生化和/或药理活性的分子形成异二聚体或异寡聚体，这些活性与相应的单体或同聚体不同。最近的体外和体内实验数据也显示了几种孤儿GPCR作为异二聚体调节单元的新功能作用以及开发异二聚体选择性临床药物的潜力。在这篇综述中，我们总结了关于GPCR异二聚化的基本和最新知识以及近期有待解决的当前问题。
