title: The expanding roles of Gβγ subunits in G protein-coupled receptor signaling and drug action.
abstract: Gβγ subunits from heterotrimeric G proteins perform a vast array of functions in cells with respect to signaling, often independently as well as in concert with Gα subunits. However, the eponymous term "Gβγ" does not do justice to the fact that 5 Gβ and 12 Gγ isoforms have evolved in mammals to serve much broader roles beyond their canonical roles in cellular signaling. We explore the phylogenetic diversity of Gβγ subunits with a view toward understanding these expanded roles in different cellular organelles. We suggest that the particular content of distinct Gβγ subunits regulates cellular activity, and that the granularity of individual Gβ and Gγ action is only beginning to be understood. Given the therapeutic potential of targeting Gβγ action, this larger view serves as a prelude to more specific development of drugs aimed at individual isoforms.
authors: Department of Pharmacology and Therapeutics, McGill University, 3655 Promenade Sir-William-Osler, Room 1303, Montréal, Québec H3G 1Y6, Canada.
authors: Shahriar M
authors: SM
authors: Khan
authors: Rory
authors: R
authors: Sleno
authors: Sarah
authors: S
authors: Gora
authors: Peter
authors: P
authors: Zylbergold
authors: Jean-Philippe
authors: JP
authors: Laverdure
authors: Jean-Claude
authors: JC
authors: Labbé
authors: Gregory J
authors: GJ
authors: Miller
authors: Terence E
authors: TE
authors: Hébert
mesh_terms: D000818:Animals; D001665:Binding Sites; D055808:Drug Discovery; D044387:GTP-Binding Protein beta Subunits / Q000737:chemistry / Q000235:genetics / Q000378:metabolism / Q000502:physiology*; D044388:GTP-Binding Protein gamma Subunits / Q000737:chemistry / Q000235:genetics / Q000378:metabolism / Q000502:physiology*; D006801:Humans; D008958:Models, Molecular; D015388:Organelles / Q000187:drug effects / Q000378:metabolism; D010802:Phylogeny; D015398:Signal Transduction / Q000187:drug effects; D054852:Small Molecule Libraries / Q000494:pharmacology; D013045:Species Specificity
chemical_list: C118981:G-protein Beta gamma; D044387:GTP-Binding Protein beta Subunits; D044388:GTP-Binding Protein gamma Subunits; D054852:Small Molecule Libraries