• Gi protein alpha subunit is a family of heterotrimeric G protein alpha subunits. (wikipedia.org)
  • A common feature of all three GPCRs is that they can couple to the G12 family of heterotrimeric G proteins [ 13 ]. (biomedcentral.com)
  • Heterotrimeric G proteins are essential mediators of G protein-coupled receptors (GPCRs) signalling to intracellular effectors. (nih.gov)
  • There are four distinct subtypes of alpha subunits in the Gi/o/z/t alpha subunit family that define four families of heterotrimeric G proteins: Gi proteins: Gi1α, Gi2α, and Gi3α Go protein: Goα (in mouse there is alternative splicing to generate Go1α and Go2α) Gz protein: Gzα Transducins (Gt proteins): Gt1α, Gt2α, Gt3α Gi1α is encoded by the gene GNAI1. (wikipedia.org)
  • Heterotrimeric G-proteins, consisting of Gα, Gβ and Gγ subunits are the major effector molecules of GPCR signaling. (biomedcentral.com)
  • The general function of Gi/o/z/t is to activate intracellular signaling pathways in response to activation of cell surface G protein-coupled receptors (GPCRs). (wikipedia.org)
  • The Transducins Gt1 and Gt2 serve to transduce signals from G protein-coupled receptors that receive light during vision. (wikipedia.org)
  • Gt3/Gustducin subunits transduce signals in the sense of taste (gustation) in taste buds by coupling to G protein-coupled receptors activated by sweet or bitter substances. (wikipedia.org)
  • Gα13 (GNA13) is the α subunit of a heterotrimeric G protein that mediates signaling through specific G protein-coupled receptors (GPCRs). (biomedcentral.com)
  • Efforts to understand the genes and signaling pathways that promote tumor invasion and metastasis have revealed that several G-protein coupled receptors (GPCRs) and their respective ligands function as metastatic drivers in breast as well other cancer types [ 2 - 6 ]. (biomedcentral.com)
  • Introduction of the Gα12-coupling BRET assay is expected to accelerate characterization of GPCR actions on this understudied G protein. (nih.gov)
  • We further showed the utility of this assay to other GPCRs by demonstrating Gα12 coupling of cholecystokinin A receptor (CCKAR). (nih.gov)
  • GPCRs function as part of a three-component system of receptor-transducer-effector. (wikipedia.org)
  • When not stimulated by a receptor, Gα is bound to GDP and to Gβγ to form the inactive G protein trimer. (wikipedia.org)
  • When the receptor binds an activating ligand outside the cell (such as a hormone or neurotransmitter), the activated receptor acts as a guanine nucleotide exchange factor to promote GDP release from and GTP binding to Gα, which drives dissociation of GTP-bound Gα from Gβγ. (wikipedia.org)
  • The Gβγ liberated by activation of Gi and Go proteins is particularly able to activate downstream signaling to effectors such as G protein-coupled inwardly-rectifying potassium channels (GIRKs). (wikipedia.org)
  • Among these, the G12 family, consisting of Gα12 and Gα13, (the products of the GNA12 and GNA13 genes, respectively) is one of the most important in the context of cancer. (biomedcentral.com)
  • There is a considerable diversity of G protein subunits that channel signals initiated by GPCRs into specific outcome. (nih.gov)
  • In particular, mammalian genomes contain 16 conserved genes encoding G protein α subunits with unique properties. (nih.gov)
  • GTP-bound Gα and Gβγ are then freed to activate their respective downstream signaling enzymes. (wikipedia.org)
  • However, our ability to study activation of G12/13 by GPCRs with the power to distinguish between the two subunits is limited. (nih.gov)
  • Of four Gα subfamilies (Gi/o, Gq, Gs and G12/13), members of the G12/13 group have received considerable attention for their roles in carcinogenesis. (nih.gov)
  • We demonstrated the utility of this assay to quantify rates of G protein activation and inactivation as well as performing dose-response studies while rank ordering signalling via individual Gα subunits. (nih.gov)
  • Pertussis toxin is an ADP-ribosylase enzyme that adds an ADP-ribose moiety to a particular cysteine residue in Giα and Goα proteins, preventing their coupling to and activation by GPCRs, thus turning off Gi and Go cell signaling pathways. (wikipedia.org)
  • The transducer in this system is a heterotrimeric G protein, composed of three subunits: a Gα protein such as Giα, and a complex of two tightly linked proteins called Gβ and Gγ in a Gβγ complex. (wikipedia.org)
  • Gi proteins primarily inhibit the cAMP dependent pathway by inhibiting adenylyl cyclase activity, decreasing the production of cAMP from ATP, which, in turn, results in decreased activity of cAMP-dependent protein kinase. (wikipedia.org)
  • Ectopic expression of miR-31 in MDA-MB-231 cells significantly reduced GNA13 mRNA and protein levels, as well as GNA13-3′-UTR-reporter activity. (biomedcentral.com)
  • Conversely, blocking miR-31 activity in MCF-10a cells induced GNA13 mRNA, protein and 3′-UTR reporter activity. (biomedcentral.com)
  • GPCRs function as part of a three-component system of receptor-transducer-effector. (wikipedia.org)
  • When not stimulated by a receptor, Gα is bound to GDP and to Gβγ to form the inactive G protein trimer. (wikipedia.org)
  • When the receptor binds an activating ligand outside the cell (such as a hormone or neurotransmitter), the activated receptor acts as a guanine nucleotide exchange factor to promote GDP release from and GTP binding to Gα, which drives dissociation of GTP-bound Gα from Gβγ. (wikipedia.org)