Abstract
Activation of phosphoinositide 3-kinase (PI-3K) is essential for insulin-stimulated translocation of GLUT4 and glucose transport in insulin target tissues. A novel p110gamma PI-3K was reported to be activated by G(i)-coupled receptors via Gbetagamma subunits. We asked whether the stimulation of G(i)-coupled receptors would trigger GLUT4 translocation and glucose uptake by the activation of Gbetagamma-dependent p110gamma PI-3K. We find that this translocation and glucose uptake can be induced by the ligand stimulation of G(i)-coupled alpha(2A) adrenergic receptor and fMet-Leu-Phe receptor in cells stably expressing these receptors. The noradrenaline ('noradrenaline')- and fMet-Leu-Phe-stimulated GLUT4 translocations were abolished by pretreatment with pertussis toxin. Pretreatment with wortmannin or genistein also inhibited the G(i)-mediated GLUT4 translocation. On ligand stimulation of these two kinds of G(i)-coupled receptor, although there was a slight increase in PtdIns(3,4,5)P(3) production, activation of either the p85/p110alpha PI-3K or Gbetagamma-dependent p110gamma PI-3K was not observed even in Chinese hamster ovary cells stably overexpressing exogenous p101/p110gamma. The G(i)-mediated GLUT4 translocation was accompanied by activation of the serine-threonine kinase Akt; the inhibitory effects of pertussis toxin, wortmannin and genistein on G(i)-mediated GLUT4 translocation paralleled their inhibitory effects on Akt activation. In contrast, the activation of some other G(i)-coupled receptors, such as prostaglandin EP3alpha receptor and platelet-activating factor receptor, did not cause either pertussis-toxin-sensitive translocation of GLUT4myc or activation of Akt kinase. These results indicate that the ligand stimulation of some G(i)-coupled receptors triggers GLUT4 translocation that occurs independently of p85/p110alpha-type and p110gamma-type PI-3Ks but might involve the activation of Akt kinase.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adrenergic alpha-Agonists / pharmacology
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Amino Acid Sequence
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Androstadienes / pharmacology
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Animals
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Biological Transport / drug effects
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CHO Cells / metabolism
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Cricetinae
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Enzyme Activation
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Enzyme Inhibitors / pharmacology
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GTP-Binding Protein alpha Subunits, Gi-Go / metabolism*
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Genes, myc
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Genistein / pharmacology
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Glucose / pharmacokinetics
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Glucose Transporter Type 4
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Molecular Sequence Data
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Monosaccharide Transport Proteins / drug effects
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Monosaccharide Transport Proteins / metabolism*
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Muscle Proteins*
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N-Formylmethionine Leucyl-Phenylalanine / pharmacology
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Norepinephrine / pharmacology
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Pertussis Toxin
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Phorbol 12,13-Dibutyrate / pharmacology
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Phosphatidylinositol 3-Kinases / metabolism*
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Phosphatidylinositol Phosphates / metabolism
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Platelet Membrane Glycoproteins / drug effects
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Platelet Membrane Glycoproteins / metabolism
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Protein Serine-Threonine Kinases*
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Proto-Oncogene Proteins / metabolism*
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Proto-Oncogene Proteins c-akt
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Receptors, Adrenergic, alpha-2 / drug effects
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Receptors, Adrenergic, alpha-2 / genetics
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Receptors, Adrenergic, alpha-2 / metabolism
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Receptors, Cell Surface*
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Receptors, Formyl Peptide
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Receptors, G-Protein-Coupled*
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Receptors, Immunologic / drug effects
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Receptors, Immunologic / genetics
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Receptors, Immunologic / metabolism
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Receptors, Peptide / drug effects
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Receptors, Peptide / genetics
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Receptors, Peptide / metabolism
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Receptors, Prostaglandin E / drug effects
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Receptors, Prostaglandin E / metabolism
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Virulence Factors, Bordetella / pharmacology
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Wortmannin
Substances
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Adrenergic alpha-Agonists
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Androstadienes
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Enzyme Inhibitors
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Glucose Transporter Type 4
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Monosaccharide Transport Proteins
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Muscle Proteins
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Phosphatidylinositol Phosphates
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Platelet Membrane Glycoproteins
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Proto-Oncogene Proteins
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Receptors, Adrenergic, alpha-2
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Receptors, Cell Surface
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Receptors, Formyl Peptide
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Receptors, G-Protein-Coupled
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Receptors, Immunologic
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Receptors, Peptide
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Receptors, Prostaglandin E
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Virulence Factors, Bordetella
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phosphatidylinositol 3,4,5-triphosphate
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platelet activating factor receptor
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Phorbol 12,13-Dibutyrate
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N-Formylmethionine Leucyl-Phenylalanine
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Genistein
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Pertussis Toxin
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Protein Serine-Threonine Kinases
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Proto-Oncogene Proteins c-akt
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GTP-Binding Protein alpha Subunits, Gi-Go
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Glucose
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Norepinephrine
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Wortmannin