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Details on Person The liganded receptor undergoes a conformational change, gen...

Class:IdSummation:751022
_displayNameThe liganded receptor undergoes a conformational change, gen...
_timestamp2025-01-24 15:26:23
created[InstanceEdit:751025] Jupe, S, 2010-05-19
literatureReference[LiteratureReference:751026] G proteins: transducers of receptor-generated signals
[LiteratureReference:751041] Signalling functions and biochemical properties of pertussis toxin-resistant G-proteins
[LiteratureReference:750995] The influence of bound GDP on the kinetics of guanine nucleotide binding to G proteins
[LiteratureReference:8949499] Genetic screens in yeast to identify mammalian nonreceptor modulators of G-protein signaling
[LiteratureReference:8949508] Receptor-independent activators of heterotrimeric G-protein signaling pathways
[LiteratureReference:8949506] Activators of G protein signaling exhibit broad functionality and define a distinct core signaling triad
[LiteratureReference:8862129] Stabilization of the GDP-bound conformation of Gialpha by a peptide derived from the G-protein regulatory motif of AGS3
[LiteratureReference:8862130] AGS3 inhibits GDP dissociation from galpha subunits of the Gi family and rhodopsin-dependent activation of transducin
[LiteratureReference:8949493] Identification and characterization of AGS4: a protein containing three G-protein regulatory motifs that regulate the activation state of Gialpha
[LiteratureReference:8949513] Oxidized human neuroglobin acts as a heterotrimeric Galpha protein guanine nucleotide dissociation inhibitor
[LiteratureReference:8949501] Identification and cDNA cloning of a novel human mosaic protein, LGN, based on interaction with G alpha i2
[LiteratureReference:8949498] Structural diversity in the RGS domain and its interaction with heterotrimeric G protein alpha-subunits
modified[InstanceEdit:8949504] Jupe, Steve, 2016-11-25
[InstanceEdit:9936591] May, Bruce, 2025-01-24
textThe liganded receptor undergoes a conformational change, generating a signal that is propagated in a manner that is not completely understood to the G-protein. This stimulates the exchange of GDP for GTP in the G-protein alpha subunit, activating the G-protein.

This event is negatively regulated by some Activators of G protein signaling (AGS) proteins, a class of proteins identified in yeast functional screens for proteins able to activate G protein signaling in the absence of a G protein–coupled receptor (GPCR) (Cismowski et al. 1999, Takesono et al. 1999). AGS proteins contain G protein regulatory (GPR) motifs (also referred to as the GoLoco motif) that bind and stabilize the Galpha subunit in its GDP-bound conformation (Mochizuki et al. 1996, Peterson et al. 2000, Cao et al. 2004, Blumer & Lanier 2014). Some RGS proteins similarly bind to Galpha preventing the exchange of GDP for GTP (Soundararajan et al. 2008).
(summation)[Reaction:379044] Liganded Gs-activating GPCR acts as a GEF for Gs [Homo sapiens]
[Reaction:380073] Liganded Gi-activating GPCR acts as a GEF for Gi [Homo sapiens]
[Reaction:749453] Liganded Gz-activating GPCR acts as a GEF for Gz [Homo sapiens]
[Reaction:751029] Liganded G12/13-activating GPCR acts as a GEF for G12/13 [Homo sapiens]
[Reaction:9660824] ADORA2B (in Ade-Rib:ADORA2B:Heterotrimeric G-protein Gs) exchanges GDP for GTP on Gs [Homo sapiens]
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