title: Dynamics of G protein effector interactions and their impact on timing and sensitivity of G protein-mediated signal transduction.
abstract: G protein coupled receptors regulate numerous cellular functions primarily via coupling to heterotrimeric G proteins and subsequent regulation of effector proteins such as ion channels, enzymes or GTP exchange factors for small G proteins. The dynamics of interactions between G protein subunits and effectors have been difficult to study particularly in a cellular context. The introduction of Förster resonance energy transfer methods into the field of GPCR research led to interesting insights into the temporal patterns of interactions between G protein subunits and their effectors. In this review we specifically focus on the interaction of Gαi subunits with adenylyl cyclases and of Gαq subunits with p63RhoGEF or G protein coupled receptor kinases type 2. Comparing the dynamics of these interactions revealed remarkable differences between different G protein effectors regarding the ability to be modulated by members of the regulator of G protein signalling protein family as well as the sensitivity towards receptor activation.
authors.affiliation: Institute for Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, Philipps-University Marburg, Karl-von-Frisch-Str. 1, 35043 Marburg, Germany.
authors.forename: Eva-Lisa
authors.initials: EL
authors.lastname: Bodmann
authors.affiliation: Institute for Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, Philipps-University Marburg, Karl-von-Frisch-Str. 1, 35043 Marburg, Germany.
authors.forename: Valerie
authors.initials: V
authors.lastname: Wolters
authors.affiliation: Institute for Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, Philipps-University Marburg, Karl-von-Frisch-Str. 1, 35043 Marburg, Germany. Electronic address: moritz.buenemann@uni-marburg.de.
authors.forename: Moritz
authors.initials: M
authors.lastname: Bünemann
mesh_terms: D000262:Adenylyl Cyclases / Q000378:metabolism*; D031541:Fluorescence Resonance Energy Transfer; D054769:G-Protein-Coupled Receptor Kinase 2 / Q000378:metabolism*; D019206:GTP-Binding Protein alpha Subunits, Gi-Go / Q000378:metabolism*; D043802:GTP-Binding Protein alpha Subunits, Gq-G11 / Q000378:metabolism*; D006801:Humans; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*; D064067:Rho Guanine Nucleotide Exchange Factors / Q000378:metabolism*; D015398:Signal Transduction
chemical_list: C475063:ARHGEF25 protein, human; D043562:Receptors, G-Protein-Coupled; D064067:Rho Guanine Nucleotide Exchange Factors; D054769:G-Protein-Coupled Receptor Kinase 2; D019206:GTP-Binding Protein alpha Subunits, Gi-Go; D043802:GTP-Binding Protein alpha Subunits, Gq-G11; D000262:Adenylyl Cyclases