Serotonin 5-HT2C receptor homodimerization is not regulated by agonist or inverse agonist treatment

European Journal of Pharmacology

Volumn 568, Issue 1-3, 2007, Pages 45-53

  Herrick Davis, Katharine ^a   Grinde, Ellinor ^a   Weaver, Barbara A ^a  

^a ALBANY MEDICAL COLLEGE   (United States)

Author keywords

Fluorescence resonance energy transfer; Homodimer; Serotonin 5 HT2C receptor

Indexed keywords

CLOZAPINE; CYAN FLUORESCENT PROTEIN; GUANINE NUCLEOTIDE BINDING PROTEIN ALPHA SUBUNIT; ISOPROTEIN; MEMBRANE PROTEIN; SEROTONIN; SEROTONIN 2 AGONIST; SEROTONIN 2C RECEPTOR; YELLOW FLUORESCENT PROTEIN;

ANXIETY DISORDER; ARTICLE; BIOLUMINESCENCE RESONANCE ENERGY TRANSFER; CELL STRAIN HEK293; CONFORMATION; CONTROLLED STUDY; DEPRESSION; DIMERIZATION; DRUG TARGETING; FLUORESCENCE RESONANCE ENERGY TRANSFER; GENE EXPRESSION; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; OBESITY; PRIORITY JOURNAL; SCHIZOPHRENIA; SIGNAL TRANSDUCTION; WESTERN BLOTTING;

ARRESTINS; CELL LINE; CELL MEMBRANE; CLOZAPINE; DIMERIZATION; FLUORESCENCE RESONANCE ENERGY TRANSFER; HUMANS; INOSITOL 1,4,5-TRISPHOSPHATE; LUCIFERASES, RENILLA; LUMINESCENT MEASUREMENTS; LUMINESCENT PROTEINS; RECEPTOR, SEROTONIN, 5-HT2C; RECOMBINANT FUSION PROTEINS; SEROTONIN; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS;

EID: 34250866786     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2007.04.030     Document Type: Article

References (52)

1. 2-adrenergic receptor dimerization in living cells using bioluminescence resonance energy transfer (BRET). Proc. Natl. Acad. Sci. 97 (2000) 3684-3689
2. Angers S., Salahpour A., and Bouvier M. Dimerization: an emerging concept for G protein-coupled receptor ontogeny and function. Annu. Rev. Pharmacol. Toxicol. 42 (2002) 409-435
3. Babcock G.J., Farzan M., and Sodroski J. Ligand-independent dimerization of CXCR4, a principal HIV-1 coreceptor. J. Biol. Chem. 278 (2003) 3378-3385
4. Baneres J.L., and Parello J. Structure-based analysis of G-protein-coupled receptor function: evidence for a novel pentameric assembly between the dimeric leukotriene B4 receptor BLT1 and the G-protein. J. Mol. Biol. 329 (2003) 815-829
5. Bastiaens P.I., Majoul I.V., Verveer P.J., Soling H.D., and Jovin T.M. Imaging the intracellular trafficking and state of the AB5 quaternary structure of cholera toxin. EMBO J. 15 (1996) 4246-4253
6. Berg K.A., Maayani S., and Clarke W.P. 5-hydroxytryptamine2C receptor activation inhibits 5-hydroxytryptamine1B-like receptor function via arachidonic acid metabolism. Mol. Pharmacol. 50 (1996) 1017-1023
7. Berthouze M., Ayoub M., Russo O., Rivail L., Sicsic S., Fischmeister R., Berque-Bestel I., Jockers R., and Lezoualc'h F. Constitutive Dimerization of Human Serotonin 5-HT4 Receptors in Living Cells (2005)
8. Burns C.M., Chu H., Rueter S.M., Hutchinson L.K., Canton H., Sanders-Bush E., and Emeson R.B. Regulation of serotonin-2C receptor G-protein coupling by RNA editing. Nature 387 (1997) 303-308
9. Chang M., Zhang L., Tam J.P., and Sanders-Bush E. Dissecting G protein-coupled receptor signaling pathways with membrane-permeable blocking peptides. Endogenous 5-HT(2C) receptors in choroid plexus epithelial cells. J. Biol. Chem. 275 (2000) 7021-7029
10. Cheng Z.J., and Miller L.J. Agonist-dependent dissociation of oligomeric complexes of G protein-coupled cholecystokinin receptors demonstrated in living cells using bioluminescence resonance energy transfer. J. Biol. Chem. 276 (2001) 8040-48047
11. Cornea A., Janovick J.A., Maya-Nunez G., and Conn P.M. Gonadotropin-releasing hormone receptor microaggregation. Rate monitored by fluorescence resonance energy transfer. J. Biol. Chem. 276 (2001) 2153-2158
12. Cvejic S., and Devi L.A. Dimerization of the delta opioid receptor: implication for a role in receptor internalization. J. Biol. Chem. 272 (1997) 26959-26964
13. Devi L.A. Heterodimerization of G-protein-coupled receptors: pharmacology, signaling and trafficking. Trends Pharmacol. Sci. 22 (2001) 532-537
14. Dinger M.C., Bader J.E., Kobor A.D., Kretzschmar A.K., and Beck-Sickinger A.G. Homodimerization of neuropeptide Y receptors investigated by fluorescence resonance energy transfer in living cells. J. Biol. Chem. 278 (2003) 10562-10571
15. Fitzgerald L.W., Iyer G., Conklin D.S., Krause C.M., Marshall A., Patterson J.P., Tran D.P., Jonak G.J., and Hartig P.R. Messenger RNA editing of the human serotonin 5-HT2C receptor. Neuropsychopharmacology 21 (1999) 82s-90s
16. Fotiadis D.M., Jastrzebska B., Philippsen A., Mu{double acute}ller D.J., Palczewski K., and Engel A. Structure of the rhodopsin dimer: a working model for G-protein-coupled receptors. Curr. Opin. Struck. Biol. 16 (2006) 252-259
17. George S.R., O'Dowd B.F., and Lee S. G-protein-coupled receptor oligomerization and its potential for drug discovery. Nat. Rev. Drug Discov. 1 (2002) 808-820
18. Goin J.C., and Nathanson N.M. Quantitative analysis of muscarinic acetylcholine receptor homo-and heterodimerization in live cells: regulation of receptor down-regulation by heterodimerization. J. Biol. Chem. 281 (2006) 5416-5425
19. Goudet C., Kniazeff J., Hlavackova V., Malhaire F., Maurel D., Archer F., Blahos J., Prezeau L., and Pin J.P. Asymmetric functioning of dimeric metabotropic glutamate receptors disclosed by positive allosteric modulators. J Biol. Chem. 280 (2005) 24380-24385
20. Grant M., Collier B., and Kumar U. Agonist-dependent dissociation of human somatostatin receptor 2 dimers: a role in receptor trafficking. J. Biol. Chem. 279 (2004) 36179-36183
21. Guo W., Shi L., and Javitch J.A. The fourth transmembrane segment forms the interface of the dopamine D2 receptor homodimer. J. Biol. Chem. 278 (2003) 4385-4388
22. Guo W., Shi L., Filizola M., Weinstein H., and Javitch J.A. Crosstalk in G protein-coupled receptors: changes at the transmembrane homodimer interface determine activation. Proc. Natl. Acad. Sci. 102 (2005) 17495-17500
23. 2C receptor RNA editing alters receptor basal activity: implications for serotonergic signal transduction. J. Neurochem. 73 (1999) 1711-1717
24. Herrick-Davis K., Grinde E., and Teitler M. Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors. J. Pharmacol. Exp. Ther. 295 (2000) 226-232
25. 2C receptor homodimers on the plasma membrane of living cells. Biochemistry 43 (2004) 13963-13971
26. Herrick-Davis K., Grinde E., Harrigan T.J., and Mazurkiewicz J.E. Inhibition of serotonin 5-hydroxytryptamine2C receptor function through heterodimerization: receptor dimers bind two molecules of ligand and one G-protein. J. Biol. Chem. 280 (2005) 40144-40151
27. Hlavackova V., Goudet C., Kniazeff J., Zikova A., Maurel D., Vol C., Trojanova J., Prezeau L., Pin J.P., and Blahos J. Evidence for a single heptahelical domain being turned on upon activation of a dimeric G-protein-coupled receptor. EMBO J. 24 (2005) 499-509
28. Hoyer D., Hannon J.P., and Martin G. Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol. Biochem. Behav. 71 (2002) 533-554
29. Jastrzebska B., Fotiadis D., Jang G.F., Stenkamp R.E., Engel A., and Palczewski K. Functional and structural characterization of rhodopsin oligomers. J. Biol. Chem. 281 (2006) 11917-11922
30. Jones B.J., and Blackburn T.P. The medical benefit of 5-HT research. Pharmacol. Biochem. Behav. 71 (2002) 555-568
31. Jones K.A., Borowsky B., Tamm J.A., Craig D.A., Durkin M.M., Dai M., Yao W.J., Johnson M., Gunwaldsen C., Huang L.Y., Tang C., Shen Q., Salon J.A., Morse K., Laz T., Smith K.E., Nagarathnam D., Noble S.A., Branchek T.A., and Gerald C. GABA(B) receptors function as a heteromeric assembly of the subunits GABA(B)R1 and GABA(B)R2. Nature 396 (1998) 674-679
32. Kenworthy A.K., and Edidin M. Distribution of a glycosylphosphatidylinositol-anchored protein at the apical surface of MDCK cells examined at a resolution of < 100 A using imaging fluorescence resonance energy transfer. J. Cell Biol. 142 (1998) 69-84
33. Kniazeff J., Bessis A.S., Maurel D., Ansanay H., Prezeau L., and Pin J.P. Closed state of both binding domains of homodimeric mGlu receptors is required for full activity. Nat. Struct. Mol. Biol. 11 (2004) 06-713
34. Kroeger K.M., Hanyaloglu A.C., Seeber R.M., Miles L.E., and Eidne K.A. Constitutive and agonist-dependent homo-oligomerization of the thyrotropin-releasing hormone receptor: detection in living cells using bioluminescence resonance energy transfer. J. Biol. Chem. 276 (2001) 12736-12743
35. Latif R., Graves P., and Davies T.F. Ligand-dependent inhibition of oligomerization at the human thyrotropin receptor. J. Biol. Chem. 277 (2002) 45059-45067
36. Lee S.P., So C.H., Rashid A.J., Varghese G., Cheng R., Lanca A.J., O'Dowd B.F., and George S.R. Dopamine D1 and D2 receptor co-activation generates a novel phospholipase C-mediated calcium signal. J. Biol. Chem. 279 (2004) 35671-35678
37. Li Z., Ichikawa J., Huang M., Prus A.J., Dai J., and Meltzer H.Y. ACP-103, a 5-HT2A/2C inverse agonist, potentiates haloperidol-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens. Psychopharmacology 183 (2005) 144-153
38. Liang Y., Fotiadis D., Filipek S., Saperstein D.A., Palczewski K., and Engel A. Organization of the G protein-coupled receptors rhodopsin and opsin in native membranes. J. Biol. Chem. 278 (2003) 21655-21662
39. Margeta-Mitrovic M., Jan Y.N., and Jan L.Y. A trafficking checkpoint controls GABA(B) receptor heterodimerization. Neuron 27 (2000) 97-106
40. McGrew L., Chang M.S., and Sanders-Bush E. Phospholipase D activation by endogenous 5-hydroxytryptamine 2C receptors is mediated by Galpha13 and pertussis toxin-insensitive Gbetagamma subunits. Mol. Pharmacol. 62 (2002) 1339-1343
41. McVey M., Ramsay D., Kellett E., Rees S., Wilson S., Pope A.J., and Milligan G. Monitoring receptor oligomerization using time-resolved fluorescence resonance energy transfer and bioluminescence resonance energy transfer: the human delta-opioid receptor displays constitutive oligomerization at the cell surface, which is not regulated by receptor occupancy. J. Biol. Chem. 276 (2001) 14092-14099
42. Mengod G., Nguyen H., Le H., Waeber C., Lubbert H., and Palacios J.M. The distribution and cellular localization of the serotonin 1C receptor mRNA in the rodent brain examined by in situ hybridization histochemistry. Comparison with receptor binding distribution. Neuroscience 35 (1990) 577-591
43. Mesnier D., and Baneres J.L. Cooperative conformational changes in a G-protein-coupled receptor dimer, the leukotriene B(4) receptor BLT1. J. Biol. Chem. 279 (2004) 49664-49670
44. 2C receptor agonists: potential for the treatment of obesity. Mol. Interv. 5 (2005) 282-291
45. Milligan G. G protein-coupled receptor dimerization: function and ligand pharmacology. Mol. Pharmacol. 66 (2004) 1-7
46. Niswender C.M., Copeland S.C., Herrick-Davis K., Emeson R.B., and Sanders-Bush E. RNA editing of the human serotonin 5-hydroxytryptamine 2C receptor silences constitutive activity. J. Biol. Chem. 274 (1999) 9472-9478
47. Rocheville M., Lange D.C., Kumar U., Sasi R., Patel R.C., and Patel Y.C. Subtypes of the somatostatin receptor assemble as functional homo- and heterodimers. J. Biol. Chem. 275 (2000) 7862-7869
48. Sanders-Bush E., and Breeding M. Serotonin1c receptor reserve in choroid plexus masks receptor subsensitivity. J. Pharmacol. Exp. Ther. 252 (1990) 984-988
49. Terrillon S., Durroux T., Mouillac B., Breit A., Ayoub M.A., Taulan M., Jockers R., Barberis C., and Bouvier M. Oxytocin and vasopressin V1a and V2 receptors form constitutive homo-and heterodimers during biosynthesis. Mol. Endocrinol. 17 (2003) 677-691
50. 2-adrenergic receptors promotes surface expression and functional activity of alpha1D-adrenergic receptors. J. Pharmacol. Exp. Ther. 313 (2005) 16-23
51. Waldhoer M., Fong J., Jones R.M., Lunzer M.M., Sharma S.K., Kostenis E., Protoghese P.D., and Whistler J.L. A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers. Proc. Natl. Acad. Sci. USA 102 (2005) 9050-9055
52. Xu Y., Piston D., and Johnson C.H. A bioluminescence resonance energy transfer (BRET) system: application to interacting circadian clock proteins. Proc. Natl. Acad. Sci. 96 (1999) 151-156