title: GPCR oligomers in pharmacology and signaling.
abstract: G protein-coupled receptors (GPCRs) represent one of the largest families of cell surface receptors, and are the target of more than half of the current therapeutic drugs on the market. When activated by an agonist, the GPCR undergoes conformational changes that facilitate its interaction with heterotrimeric G proteins, which then relay signals to downstream intracellular effectors. Although GPCRs were thought to function as monomers, many studies support the hypothesis that G protein coupling involves the formation of GPCR homo- and/or hetero-complexes. These complex systems have been suggested to exhibit specific signaling cascades, pharmacological, internalization, and recycling properties. In this review, we summarize recent advances in our understanding of the structure, function and dynamics of GPCR complexes, as well as the findings obtained in animal models.
authors: Departments of Psychiatry and Neurology, Friedman Brain Institute, Mount Sinai School of Medicine, New York, NY, USA. Javier.Maeso@mssm.edu
authors: Javier
authors: J
authors: González-Maeso
references: Curr Opin Pharmacol. 2010 Feb;10(1):23-9
references: 19850521
references: J Biol Chem. 2003 Feb 14;278(7):4385-8
references: 12496294
references: Science. 2000 Aug 4;289(5480):739-45
references: 10926528
references: Br J Pharmacol. 2006 Jan;147 Suppl 1:S46-55
references: 16402120
references: J Biol Chem. 2007 May 18;282(20):14875-81
references: 17395586
references: J Neurosci. 2001 Feb 15;21(4):1203-10
references: 11160390
references: Biochem Biophys Res Commun. 1982 Nov 16;109(1):21-9
references: 6297476
references: Nat Chem Biol. 2009 Mar;5(3):131-4
references: 19219011
references: Trends Neurosci. 2009 Apr;32(4):225-32
references: 19269047
references: Proc Natl Acad Sci U S A. 2001 Dec 4;98(25):14649-54
references: 11724956
references: Proc Natl Acad Sci U S A. 1983 Jan;80(1):156-9
references: 6571990
references: EMBO J. 2009 Nov 4;28(21):3315-28
references: 19763081
references: Mol Psychiatry. 2002;7(7):755-67
references: 12192620
references: Pharmacol Rev. 2007 Mar;59(1):5-13
references: 17329545
references: Eur J Pharmacol. 1992 Oct 1;227(2):139-46
references: 1358662
references: Biochem Biophys Res Commun. 1983 Nov 15;116(3):1070-5
references: 6316964
references: J Biol Chem. 2002 Dec 6;277(49):47748-55
references: 12356766
references: J Biol Chem. 1980 Aug 10;255(15):7108-17
references: 6248546
references: Proc Natl Acad Sci U S A. 2005 Nov 29;102(48):17495-500
references: 16301531
references: Science. 2010 Nov 19;330(6007):1066-71
references: 20929726
references: Nature. 2007 Nov 15;450(7168):383-7
references: 17952055
references: Biochemistry. 1999 Oct 5;38(40):13263-9
references: 10529199
references: Proc Natl Acad Sci U S A. 2010 Feb 9;107(6):2693-8
references: 20133736
references: EMBO J. 2011 Jan 5;30(1):32-42
references: 21063387
references: Nat Chem Biol. 2010 Jul;6(7):541-8
references: 20512139
references: Med Biol. 1982 Aug;60(4):183-90
references: 6128444
references: Nat Chem Biol. 2008 Feb;4(2):126-31
references: 18193048
references: Mol Pharmacol. 2003 Dec;64(6):1317-24
references: 14645661
references: Proc Natl Acad Sci U S A. 1991 Aug 15;88(16):7238-41
references: 1678519
references: Neuron. 2007 Feb 1;53(3):439-52
references: 17270739
references: Biochem Biophys Res Commun. 1975 Jun 16;64(4):1160-8
references: 1137592
references: Arch Gen Psychiatry. 1990 Mar;47(3):213-9
references: 1968328
references: EMBO J. 2008 Sep 3;27(17):2293-304
references: 18668123
references: Nat Rev Mol Cell Biol. 2008 Jan;9(1):60-71
references: 18043707
references: Trends Pharmacol Sci. 2010 Nov;31(11):499-508
references: 20870299
references: Mol Pharmacol. 1980 Jan;17(1):14-23
references: 6104284
references: Mol Pharmacol. 1991 Feb;39(2):211-21
references: 1899905
references: Nature. 2011 Jan 13;469(7329):175-80
references: 21228869
references: Neurosci Lett. 2011 Apr 15;493(3):76-9
references: 21276828
references: Nat Chem Biol. 2009 Sep;5(9):688-95
references: 19648932
references: J Biol Chem. 2002 May 3;277(18):15795-800
references: 11859079
references: Mol Pharmacol. 2007 Apr;71(4):1015-29
references: 17220353
references: Nature. 2008 Mar 6;452(7183):93-7
references: 18297054
references: Nature. 1999 Jun 17;399(6737):697-700
references: 10385123
references: Biol Psychiatry. 2010 Nov 1;68(9):869-72
references: 20864091
references: Br J Pharmacol. 2009 Sep;158(1):5-14
references: 19309353
references: Annu Rev Physiol. 1998;60:461-96
references: 9558473
references: Med Biol. 1980 Aug;58(4):182-7
references: 6167826
references: Nat Chem Biol. 2010 Aug;6(8):587-94
references: 20622858
references: CNS Neurol Disord Drug Targets. 2010 Nov;9(5):636-50
references: 20632964
references: Mini Rev Med Chem. 2008 Sep;8(10):996-1005
references: 18782052
references: Nat Methods. 2009 Mar;6(3):225-30
references: 19234451
references: Psychopharmacology (Berl). 1994 Jun;115(1-2):135-40
references: 7862885
references: Proc Natl Acad Sci U S A. 1993 Apr 1;90(7):3103-7
references: 8385357
references: Brain Res. 1995 Jun 5;682(1-2):245-50
references: 7552322
references: Nat Biotechnol. 2003 Jul;21(7):807-12
references: 12808462
references: Trends Pharmacol Sci. 2010 Mar;31(3):124-30
references: 20060175
references: Nature. 2009 May 21;459(7245):356-63
references: 19458711
references: Nat Neurosci. 2010 May;13(5):622-9
references: 20383137
references: Nat Struct Mol Biol. 2004 Aug;11(8):706-13
references: 15235591
references: Mol Pharmacol. 2004 Nov;66(5):1123-37
references: 15304550
references: Nat Methods. 2008 Jun;5(6):561-7
references: 18488035
references: Sci Signal. 2010 Jul 20;3(131):ra54
references: 20647592
references: EMBO J. 2009 Aug 5;28(15):2195-208
references: 19590495
references: Proc Natl Acad Sci U S A. 2010 Feb 2;107(5):2319-24
references: 20080658
references: Proc Natl Acad Sci U S A. 2007 May 1;104(18):7682-7
references: 17452637
references: Mol Pharmacol. 2009 Jun;75(6):1296-9
references: 19273553
references: J Biol Chem. 2004 Aug 6;279(32):33390-7
references: 15155738
references: J Pharmacol Exp Ther. 2000 Jan;292(1):2-7
references: 10604925
references: Mol Psychiatry. 2000 May;5(3):308-15
references: 10889534