期刊
TRENDS IN PHARMACOLOGICAL SCIENCES
卷 39, 期 7, 页码 672-684出版社
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tips.2018.04.002
关键词
-
资金
- NIH [EY011500, GM077561, GM109955, R35 GM122491, NS065868, DA030103]
Until the late 1990s, class A G protein-coupled receptors (GPCRs) were believed to function as monomers. Indirect evidence that they might internalize or even signal as dimers has emerged, along with proof that class C GPCRs are obligatory dimers. Crystal structures of GPCRs and their much larger binding partners were consistent with the idea that two receptors might engage a single G protein, GRK, or arrestin. However, recent biophysical, biochemical, and structural evidence invariably suggests that a single GPCR binds G proteins, GRKs, and arrestins. Here we review existing evidence of the stoichiometry of GPCR interactions with signal transducers and discuss potential biological roles of class A GPCR oligomers, including proposed homo- and heterodimers.
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