5-HT receptor-associated protein networks: New targets for drug discovery in psychiatric disorders?

Current Drug Targets

Volumn 13, Issue 1, 2012, Pages 28-52

  Marin, Philippe ^a,b   Becamel, Carine ^a,b   Dumuis, Aline ^a,b   Bockaert, Joël ^a,b  

^a INSTITUT DE GÉNOMIQUE FONCTIONNELLE   (France)

^b UNIV MONTPELLIER   (France)

Author keywords

arrestin; 5 HT receptor; Calmodulin; PDZ protein; Protein kinase; Signalling; Targeting; Trafficking

Indexed keywords

ANTIDEPRESSANT AGENT; BETA ACTIN; BETA ARRESTIN; CATION CHANNEL; G PROTEIN COUPLED RECEPTOR; G PROTEIN COUPLED RECEPTOR INTERACTING PROTEIN; G PROTEIN COUPLED RECEPTOR KINASE; METABOTROPIC RECEPTOR; MITOGEN ACTIVATED PROTEIN KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE 3; NEUROLEPTIC AGENT; PROTEIN TYROSINE KINASE; PSYCHEDELIC AGENT; SEROTONIN; SEROTONIN 1A RECEPTOR; SEROTONIN 1B RECEPTOR; SEROTONIN 1D RECEPTOR; SEROTONIN 1E RECEPTOR; SEROTONIN 1F RECEPTOR; SEROTONIN 2A RECEPTOR; SEROTONIN 2B RECEPTOR; SEROTONIN 2C RECEPTOR; SEROTONIN 3 RECEPTOR; SEROTONIN 4 RECEPTOR; SEROTONIN 5 RECEPTOR; SEROTONIN 6 RECEPTOR; SEROTONIN 7 RECEPTOR; SEROTONIN RECEPTOR; SEROTONIN RECEPTOR ASSOCIATED PROTEIN; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ADDICTION; ANXIETY DISORDER; ARTICLE; DEPRESSION; DRUG TARGETING; HUMAN; MENTAL DISEASE; NONHUMAN; PROTEIN FAMILY; PROTEOMICS; PSYCHOSIS; SEROTONINERGIC SYSTEM; SEROTONINERGIC TRANSMISSION; SIGNAL TRANSDUCTION; TWO HYBRID SYSTEM;

ANIMALS; ANTIPSYCHOTIC AGENTS; DRUG DELIVERY SYSTEMS; DRUG DISCOVERY; HUMANS; MENTAL DISORDERS; PROTEIN INTERACTION MAPS; RECEPTORS, SEROTONIN;

EID: 84855823925     PISSN: 13894501     EISSN: 18735592     Source Type: Journal    
DOI: 10.2174/138945012798868498     Document Type: Article

References (210)

1. Hardeland R. Melatonin and 5-methoxytryptamine in nonmetazoans. Reprod Nutr Dev 1999; 39: 399-408.
2. Strakhovskaia MG, Serdalina AM, Fraikin G. [Effect of the photoinduced synthesis of serotonin on the photoreactivation of Saccharomyces cerevisiae yeasts]. Nauchnye Doki Vyss Shkoly Biol Nauki 1983: 25-8.
3. Hajj-Ali I, Anctil M. Characterization of a serotonin receptor in the cnidarian Renilla koellikeri: a radiobinding analysis. Neurochem Int 1997; 31: 83-93.
4. Kroeze WK, Roth BL. Molecular Biology and Genomic Organization of G Protein-coupled serotonin receptors. In: Neve KA, Ed. Totowa: Humana Press; 2006.
5. Bockaert J, Claeysen S, Dumuis A, Marin P. Classification and signaling characteristics of 5-HT receptors. In: Müller CP, Jacobs BL, Eds. Handbook of behavioural neurobiology of serotonin: Elsevier; 2010. p. 103-22.
6. Fitzgerald LW, Iyer G, Conklin DS, et al. Messenger RNA editing of the human serotonin 5-HT2C receptor. Neuropsychopharmacology 1999; 21: 82S-90S.
7. Burns CM, Chu H, Rueter SM, et al. Regulation of serotonin-2C receptor G-protein coupling by RNA editing. Nature 1997; 387: 303-8.
8. Bockaert J, Roussignol G, Becamel C, et al. GPCR-interacting proteins (GIPs): nature and functions. Biochem Soc Trans 2004; 32: 851-5.
9. Bockaert J, Perroy J, Becamel C, Marin P, Fagni L. GPCR interacting proteins (GIPs) in the nervous system: Roles in physiology and pathologies. Annu Rev Pharmacol Toxicol 2010; 50: 89-109.
10. Bockaert J, Marin P, Dumuis A, Fagni L. The 'magic tail' of G protein-coupled receptors: an anchorage for functional protein networks. FEBS Lett 2003; 546: 65-72.
11. Ullmer C, Schmuck K, Figge A, Lubbert H. Cloning and characterization of MUPP1, a novel PDZ domain protein. FEBS Lett 1998; 424: 63-8.
12. Carrel D, Masson J, Al Awabdh S, et al. Targeting of the 5-HT1A serotonin receptor to neuronal dendrites is mediated by Yif1B. J Neurosci 2008; 28: 8063-73.
13. Yun HM, Kim S, Kim HJ, et al. The novel cellular mechanism of human 5-HT6 receptor through an interaction with Fyn. J Biol Chem 2007; 282: 5496-505.
14. Yun HM, Baik JH, Kang IS, Jin C, Rhim H. Physical interaction of Jab1 with human serotonin 6 G-protein-coupled receptor and their possible roles in cell survival. J Biol Chem 2010; 285: 10016-29.
15. Dirnberger D, Messerschmid M, Baumeister R. An optimized splitubiquitin cDNA-library screening system to identify novel interactors of the human Frizzled 1 receptor. Nucleic Acids Res 2008; 36: e37.
16. Becamel C, Alonso G, Galeotti N, et al. Synaptic multiprotein complexes associated with 5-HT(2C) receptors: a proteomic approach. EMBO J 2002; 21: 2332-42.
17. Becamel C, Galeotti N, Poncet J, et al. A proteomic approach based on peptide affinity chromatography, 2-dimensional electrophoresis and mass spectrometry to identify multiprotein complexes interacting with membrane-bound receptors. Biol Proced Online 2002; 4: 94-104.
18. Becamel C, Gavarini S, Chanrion B, et al. The serotonin 5-HT2A and 5-HT2C receptors interact with specific sets of PDZ proteins. J Biol Chem 2004; 279: 20257-66.
19. Joubert L, Hanson B, Barthet G, et al. New sorting nexin (SNX27) and NHERF specifically interact with the 5-HT4(a) receptor splice variant: roles in receptor targeting. J Cell Sci 2004; 117: 5367-79.
20. Daulat AM, Maurice P, Jockers R. Recent methodological advances in the discovery of GPCR-associated protein complexes. Trends Pharmacol Sci 2009; 30: 72-8.
21. Farr CD, Gafken PR, Norbeck AD, et al. Proteomic analysis of native metabotropic glutamate receptor 5 protein complexes reveals novel molecular constituents. J Neurochem 2004; 91: 438-50.
22. Schwenk J, Metz M, Zolles G, et al. Native GABA(B) receptors are heteromultimers with a family of auxiliary subunits. Nature 2010; 465: 231-5.
23. Fernandez E, Collins MO, Uren RT, et al. Targeted tandem affinity purification of PSD-95 recovers core postsynaptic complexes and schizophrenia susceptibility proteins. Mol Syst Biol 2009; 5: 269.
24. Paquet M, Asay MJ, Fam SR, et al. The PDZ scaffold NHERF-2 interacts with mGluR5 and regulates receptor activity. J Biol Chem 2006; 281: 29949-61.
25. Fam SR, Paquet M, Castleberry AM, et al. P2Y1 receptor signaling is controlled by interaction with the PDZ scaffold NHERF-2. Proc Natl Acad Sci USA 2005; 102: 8042-7.
26. He J, Bellini M, Inuzuka H, et al. Proteomic analysis of beta1-adrenergic receptor interactions with PDZ scaffold proteins. J Biol Chem 2006; 281: 2820-7.
27. Hoyer D, Hannon JP, Martin GR. Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol Biochem Behav 2002; 71: 533-54.
28. Bockaert J, Claeysen S, Becamel C, Dumuis A, Marin P. Neuronal 5-HT metabotropic receptors: fine-tuning of their structure, signaling, and roles in synaptic modulation. Cell Tissue Res 2006; 326: 553-72.
29. Kobilka BK, Frielle T, Collins S, et al. An intronless gene encoding a potential member of the family of receptors coupled to guanine nucleotide regulatory proteins. Nature 1987; 329: 75-9.
30. Fargin A, Raymond JR, Lohse MJ, Kobilka BK, Caron MG, Lefkowitz RJ. The genomic clone G-21 which resembles a betaadrenergic receptor sequence encodes the 5-HT1A receptor. Nature 1988; 335: 358-60.
31. Lanfumey L, Hamon M. 5-HT1 receptors. Curr Drug Targets CNS Neurol Disord 2004; 3: 1-10.
32. Riad M, Garcia S, Watkins KC, et al. Somatodendritic localization of 5-HT1A and preterminal axonal localization of 5-HT1B serotonin receptors in adult rat brain. J Comp Neurol 2000; 417: 181-94.
33. Kia HK, Miquel MC, Brisorgueil MJ, et al. Immunocytochemical localization of serotonin1A receptors in the rat central nervous system. J Comp Neurol 1996; 365: 289-305.
34. Parks CL, Robinson PS, Sibille E, Shenk T, Toth M. Increased anxiety of mice lacking the serotonin1A receptor. Proc Natl Acad Sci USA 1998; 95: 10734-9.
35. Artigas F, Romero L, de Montigny C, Blier P. Acceleration of the effect of selected antidepressant drugs in major depression by 5-HT1A antagonists. Trends Neurosci 1996; 19: 378-83.
36. Artigas F, Celada P, Laruelle M, Adell A. How does pindolol improve antidepressant action? Trends Pharmacol Sci 2001; 22: 224-8.
37. Radley JJ, Jacobs BL. 5-HT1A receptor antagonist administration decreases cell proliferation in the dentate gyrus. Brain Res 2002; 955: 264-7.
38. Raymond JR, Mukhin YV, Gelasco A, et al. Multiplicity of mechanisms of serotonin receptor signal transduction. Pharmacol Ther 2001; 92: 179-212.
39. Andrade R, Malenka RC, Nicoll RA. A G protein couples serotonin and GABAB receptors to the same channels in hippocampus. Science 1986; 234: 1261-5.
40. Innis RB, Nestler EJ, Aghajanian GK. Evidence for G protein mediation of serotonin-and GABAB-induced hyperpolarization of rat dorsal raphe neurons. Brain Res 1988; 459: 27-36.
41. Sodickson DL, Bean BP. Neurotransmitter activation of inwardly rectifying potassium current in dissociated hippocampal CA3 neurons: interactions among multiple receptors. J Neurosci 1998; 18: 8153-62.
42. Oleskevich S. G alpha o1 decapeptide modulates the hippocampal 5-HT1A potassium current. J Neurophysiol 1995; 74: 2189-93.
43. la Cour CM, El Mestikawy S, Hanoun N, Hamon M, Lanfumey L. Regional differences in the coupling of 5-hydroxytryptamine-1A receptors to G proteins in the rat brain. Mol Pharmacol 2006; 70: 1013-21.
44. Della Rocca GJ, Mukhin YV, Garnovskaya MN, et al. Serotonin 5-HT1A receptor-mediated Erk activation requires calcium/ calmodulin-dependent receptor endocytosis. J Biol Chem 1999; 274: 4749-53.
45. Crane JW, Shimizu K, Carrasco GA, et al. 5-HT1A receptors mediate (+)8-OH-DPAT-stimulation of extracellular signalregulated kinase (MAP kinase) in vivo in rat hypothalamus: time dependence and regional differences. Brain Res 2007; 1183: 51-9.
46. Chaput Y, de Montigny C, Blier P. Effects of a selective 5-HT reuptake blocker, citalopram, on the sensitivity of 5-HT autoreceptors: electrophysiological studies in the rat brain. Naunyn Schmiedebergs Arch Pharmacol 1986; 333: 342-8.
47. Le Poul E, Boni C, Hanoun N, et al. Differential adaptation of brain 5-HT1A and 5-HT1B receptors and 5-HT transporter in rats treated chronically with fluoxetine. Neuropharmacology 2000; 39: 110-22.
48. Mannoury la Cour C, Boni C, Hanoun N, Lesch KP, Hamon M, Lanfumey L. Functional consequences of 5-HT transporter gene disruption on 5-HT(1a) receptor-mediated regulation of dorsal raphe and hippocampal cell activity. J Neurosci 2001; 21: 2178-85.
49. Turner JH, Garnovskaya MN, Raymond JR. Serotonin 5-HT1A receptor stimulates c-Jun N-terminal kinase and induces apoptosis in Chinese hamster ovary fibroblasts. Biochim Biophys Acta 2007; 1773: 391-9.
50. 2+-calmodulin and janus kinase 2 are required for activation of sodium-proton exchange by the Gi-coupled 5-hydroxytryptamine 1a receptor. J Pharmacol Exp Ther 2007; 320: 314-22.
51. Sari Y. Serotonin1B receptors: from protein to physiological function and behavior. Neurosci Biobehav Rev 2004; 28: 565-82.
52. Gingrich JA, Hen R. Dissecting the role of the serotonin system in neuropsychiatric disorders using knockout mice. Psychopharmacology (Berl) 2001; 155: 1-10.
53. Ferrari MD, Goadsby PJ, Roon KI, Lipton RB. Triptans (serotonin, 5-HT1B/1D agonists) in migraine: detailed results and methods of a meta-analysis of 53 trials. Cephalalgia 2002; 22: 633-58.
54. Xie Z, Lee SP, O'Dowd BF, George SR. Serotonin 5-HT1B and 5-HT1D receptors form homodimers when expressed alone and heterodimers when co-expressed. FEBS Lett 1999; 456: 63-7.
55. Cutrer FM, Yu XJ, Ayata G, Moskowitz MA, Waeber C. Effects of PNU-109,291, a selective 5-HT1D receptor agonist, on electrically induced dural plasma extravasation and capsaicin-evoked c-fos immunoreactivity within trigeminal nucleus caudalis. Neuropharmacology 1999; 38: 1043-53.
56. Mengod g, Cortes R, Vilaro M, Hoyer D. Distribution of 5-HT receptors in the central nervous system. In: Müller CP, Jacobs BL, editors. Handbook of behavioural neurobiology of serotonin: Elsevier; 2010. p. 123-32.
57. Leysen JE. 5-HT2 receptors. Curr Drug Targets CNS Neurol Disord 2004; 3: 11-26.
58. Cornea-Hebert V, Riad M, Wu C, Singh SK, Descarries L. Cellular and subcellular distribution of the serotonin 5-HT2A receptor in the central nervous system of adult rat. J Comp Neurol 1999; 409: 187-209.
59. Cornea-Hebert V, Watkins KC, Roth BL, et al. Similar ultrastructural distribution of the 5-HT(2A) serotonin receptor and microtubule-associated protein MAP1A in cortical dendrites of adult rat. Neuroscience 2002; 113: 23-35.
60. Miner LA, Backstrom JR, Sanders-Bush E, Sesack SR. Ultrastructural localization of serotonin2A receptors in the middle layers of the rat prelimbic prefrontal cortex. Neuroscience 2003; 116: 107-17.
61. Jakab RL, Goldman-Rakic PS. 5-Hydroxytryptamine2A serotonin receptors in the primate cerebral cortex: possible site of action of hallucinogenic and antipsychotic drugs in pyramidal cell apical dendrites. Proc Natl Acad Sci USA 1998; 95: 735-40.
62. Nocjar C, Roth BL, Pehek EA. Localization of 5-HT(2A) receptors on dopamine cells in subnuclei of the midbrain A10 cell group. Neuroscience 2002; 111: 163-76.
63. Cohen J, Iuvone PM, Neff NH. Neuroleptic drugs activate tyrosine hydroxylase of retinal amacrine cells. J Pharmacol Exp Ther 1981; 218: 390-4.
64. Cook EH, Jr., Fletcher KE, Wainwright M, Marks N, Yan SY, Leventhal BL. Primary structure of the human platelet serotonin 5-HT2A receptor: identify with frontal cortex serotonin 5-HT2A receptor. J Neurochem 1994; 63: 465-9.
65. Garnovskaya MN, Nebigil CG, Arthur JM, Spurney RF, Raymond JR. 5-Hydroxytryptamine2A receptors expressed in rat renal mesangial cells inhibit cyclic AMP accumulation. Mol Pharmacol 1995; 48: 230-7.
66. Lesurtel M, Graf R, Aleil B, et al. Platelet-derived serotonin mediates liver regeneration. Science 2006; 312: 104-7.
67. Guillet-Deniau I, Burnol AF, Girard J. Identification and localization of a skeletal muscle secrotonin 5-HT2A receptor coupled to the Jak/STAT pathway. J Biol Chem 1997; 272: 14825-9.
68. Harvey JA. Role of the serotonin 5-HT(2A) receptor in learning. Learn Mem 2003; 10: 355-62.
69. Roth BL, Willins DL, Kristiansen K, Kroeze WK. 5-Hydroxytryptamine2-family receptors (5-hydroxytryptamine2A, 5-hydroxytryptamine2B, 5-hydroxytryptamine2C): where structure meets function. Pharmacol Ther 1998; 79: 231-57.
70. Li P, Kerchner GA, Sala C, et al. AMPA receptor-PDZ interactions in facilitation of spinal sensory synapses. Nat Neurosci 1999; 2: 972-7.
71. Li P, Zhuo M. Silent glutamatergic synapses and nociception in mammalian spinal cord. Nature 1998; 393: 695-8.
72. Millan MJ. Serotonin 5-HT2C receptors as a target for the treatment of depressive and anxious states: focus on novel therapeutic strategies. Therapie 2005; 60: 441-60.
73. Millan MJ. The neurobiology and control of anxious states. Prog Neurobiol 2003; 70: 83-244.
74. Millan MJ. Multi-target strategies for the improved treatment of depressive states: Conceptual foundations and neuronal substrates, drug discovery and therapeutic application. Pharmacol Ther 2006; 110: 135-370.
75. Weisstaub NV, Zhou M, Lira A, et al. Cortical 5-HT2A receptor signaling modulates anxiety-like behaviors in mice. Science 2006; 313: 536-40.
76. Celada P, Puig M, Amargos-Bosch M, Adell A, Artigas F. The therapeutic role of 5-HT1A and 5-HT2A receptors in depression. J Psychiatry Neurosci 2004; 29: 252-65.
77. Aghajanian GK, Marek GJ. Serotonin and hallucinogens. Neuropsychopharmacology 1999; 21: 16S-23S.
78. Meltzer HY, Matsubara S, Lee JC. Classification of typical and atypical antipsychotic drugs on the basis of dopamine D-1, D-2 and serotonin2 pKi values. J Pharmacol Exp Ther 1989; 251: 238-46.
79. Newman-Tancredi A, Cussac D, Marini L, Millan MJ. Antibody capture assay reveals bell-shaped concentration-response isotherms for h5-HT(1A) receptor-mediated Galpha(i3) activation: conformational selection by high-efficacy agonists, and relationship to trafficking of receptor signaling. Mol Pharmacol 2002; 62: 590-601.
80. Gonzalez-Maeso J, Weisstaub NV, Zhou M, et al. Hallucinogens recruit specific cortical 5-HT(2A) receptor-mediated signaling pathways to affect behavior. Neuron 2007; 53: 439-52.
81. Banes A, Florian JA, Watts SW. Mechanisms of 5-hydroxytryptamine(2A) receptor activation of the mitogenactivated protein kinase pathway in vascular smooth muscle. J Pharmacol Exp Ther 1999; 291: 1179-87.
82. Banes AK, Shaw SM, Tawfik A, et al. Activation of the JAK/STAT pathway in vascular smooth muscle by serotonin. Am J Physiol Cell Physiol 2005; 288: C805-12.
83. Tournois C, Mutel V, Manivet P, Launay JM, Kellermann O. Cross-talk between 5-hydroxytryptamine receptors in a serotonergic cell line. Involvement of arachidonic acid metabolism. J Biol Chem 1998; 273: 17498-503.
84. Quinn JC, Johnson-Farley NN, Yoon J, Cowen DS. Activation of extracellular-regulated kinase by 5-hydroxytryptamine(2A) receptors in PC12 cells is protein kinase C-independent and requires calmodulin and tyrosine kinases. J Pharmacol Exp Ther 2002; 303: 746-52.
85. Tsuchioka M, Takebayashi M, Hisaoka K, Maeda N, Nakata Y. Serotonin (5-HT) induces glial cell line-derived neurotrophic factor (GDNF) mRNA expression via the transactivation of fibroblast growth factor receptor 2 (FGFR2) in rat C6 glioma cells. J Neurochem 2008; 106: 244-57.
86. Carr DB, Cooper DC, Ulrich SL, Spruston N, Surmeier DJ. Serotonin receptor activation inhibits sodium current and dendritic excitability in prefrontal cortex via a protein kinase C-dependent mechanism. J Neurosci 2002; 22: 6846-55.
87. Arvanov VL, Liang X, Magro P, Roberts R, Wang RY. A pre-and postsynaptic modulatory action of 5-HT and the 5-HT2A, 2C receptor agonist DOB on NMDA-evoked responses in the rat medial prefrontal cortex. Eur J Neurosci 1999; 11: 2917-34.
88. Arvanov VL, Liang X, Russo A, Wang RY. LSD and DOB: interaction with 5-HT2A receptors to inhibit NMDA receptormediated transmission in the rat prefrontal cortex. Eur J Neurosci 1999; 11: 3064-72.
89. Aghajanian GK, Marek GJ. Serotonin, via 5-HT2A receptors, increases EPSCs in layer V pyramidal cells of prefrontal cortex by an asynchronous mode of glutamate release. Brain Res 1999; 825: 161-71.
90. Villalobos C, Beique JC, Gingrich JA, Andrade R. Serotonergic regulation of calcium-activated potassium currents in rodent prefrontal cortex. Eur J Neurosci 2005; 22: 1120-6.
91. Jones KA, Srivastava DP, Allen JA, Strachan RT, Roth BL, Penzes P. Rapid modulation of spine morphology by the 5-HT2A serotonin receptor through kalirin-7 signaling. Proc Natl Acad Sci USA 2009; 106: 19575-80.
92. Choi DS, Birraux G, Launay JM, Maroteaux L. The human serotonin 5-HT2B receptor: pharmacological link between 5-HT2 and 5-HT1D receptors. FEBS Lett 1994; 352: 393-9.
93. Nebigil CG, Choi DS, Dierich A, et al. Serotonin 2B receptor is required for heart development. Proc Natl Acad Sci USA 2000; 97: 9508-13.
94. Nebigil CG, Maroteaux L. Functional consequence of serotonin/5-HT2B receptor signaling in heart: role of mitochondria in transition between hypertrophy and heart failure? Circulation 2003; 108: 902-8.
95. Choi DS, Ward SJ, Messaddeq N, Launay JM, Maroteaux L. 5-HT2B receptor-mediated serotonin morphogenetic functions in mouse cranial neural crest and myocardiac cells. Development 1997; 124: 1745-55.
96. Nebigil CG, Jaffre F, Messaddeq N, et al. Overexpression of the serotonin 5-HT2B receptor in heart leads to abnormal mitochondrial function and cardiac hypertrophy. Circulation 2003; 107: 3223-9.
97. Glusa E, Pertz HH. Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT(2B) receptors. Br J Pharmacol 2000; 130: 692-8.
98. Launay JM, Herve P, Peoc'h K, et al. Function of the serotonin 5-hydroxytryptamine 2B receptor in pulmonary hypertension. Nat Med 2002; 8: 1129-35.
99. Manivet P, Mouillet-Richard S, Callebert J, et al. PDZ-dependent activation of nitric-oxide synthases by the serotonin 2B receptor. J Biol Chem 2000; 275: 9324-31.
100. Nebigil CG, Etienne N, Messaddeq N, Maroteaux L. Serotonin is a novel survival factor of cardiomyocytes: mitochondria as a target of 5-HT2B receptor signaling. FASEB J 2003; 17: 1373-5.
101. Abramowski D, Rigo M, Duc D, Hoyer D, Staufenbiel M. Localization of the 5-hydroxytryptamine2C receptor protein in human and rat brain using specific antisera. Neuropharmacology 1995; 34: 1635-45.
102. Wacker DA, Miller KJ. Agonists of the serotonin 5-HT2C receptor: preclinical and clinical progression in multiple diseases. Curr Opin Drug Discov Devel 2008; 11: 438-45.
103. Sanders-Bush E, Breeding M. Putative selective 5-HT-2 antagonists block serotonin 5-HT-1c receptors in the choroid plexus. J Pharmacol Exp Ther 1988; 247: 169-73.
104. McGrew L, Chang MS, Sanders-Bush E. Phospholipase D activation by endogenous 5-hydroxytryptamine 2C receptors is mediated by Galpha13 and pertussis toxin-insensitive Gbetagamma subunits. Mol Pharmacol 2002; 62: 1339-43.
105. Cussac D, Newman-Tancredi A, Duqueyroix D, Pasteau V, Millan MJ. Differential activation of Gq/11 and Gi(3) proteins at 5-hydroxytryptamine(2C) receptors revealed by antibody capture assays: influence of receptor reserve and relationship to agonistdirected trafficking. Mol Pharmacol 2002; 62: 578-89.
106. Labasque M, Reiter E, Becamel C, Bockaert J, Marin P. Physical interaction of calmodulin with the 5-hydroxytryptamine2C receptor C-terminus is essential for G protein-independent, arrestindependent receptor signaling. Mol Biol Cell 2008; 19: 4640-50.
107. Berg KA, Clarke WP, Cunningham KA, Spampinato U. Finetuning serotonin2c receptor function in the brain: molecular and functional implications. Neuropharmacology 2008; 55: 969-76.
108. Marion S, Weiner DM, Caron MG. RNA editing induces variation in desensitization and trafficking of 5-hydroxytryptamine 2c receptor isoforms. J Biol Chem 2004; 279: 2945-54.
109. Berg KA, Harvey JA, Spampinato U, Clarke WP. Physiological relevance of constitutive activity of 5-HT2A and 5-HT2C receptors. Trends Pharmacol Sci 2005; 26: 625-30.
110. Gurevich I, Englander MT, Adlersberg M, Siegal NB, Schmauss C. Modulation of serotonin 2C receptor editing by sustained changes in serotonergic neurotransmission. J Neurosci 2002; 22: 10529-32.
111. Englander MT, Dulawa SC, Bhansali P, Schmauss C. How stress and fluoxetine modulate serotonin 2C receptor pre-mRNA editing. J Neurosci 2005; 25: 648-51.
112. Kishore S, Stamm S. The snoRNA HBII-52 regulates alternative splicing of the serotonin receptor 2C. Science 2006; 311: 230-2.
113. Bockaert J, Claeysen S, Compan V, Dumuis A. 5-HT(4) receptors: history, molecular pharmacology and brain functions. Neuropharmacology 2008; 55: 922-31.
114. Bockaert J, Claeysen S, Compan V, Dumuis A. 5-HT4 receptors. Curr Drug Targets CNS Neurol Disord 2004; 3: 39-51.
115. Lucas G, Rymar VV, Du J, et al. Serotonin(4) (5-HT(4) receptor agonists are putative antidepressants with a rapid onset of action. Neuron 2007; 55: 712-25.
116. Jean A, Conductier G, Manrique C, et al. Anorexia induced by activation of serotonin 5-HT4 receptors is mediated by increases in CART in the nucleus accumbens. Proc Natl Acad Sci USA 2007; 104: 16335-40.
117. Liu MT, Kuan YH, Wang J, Hen R, Gershon MD. 5-HT4 receptormediated neuroprotection and neurogenesis in the enteric nervous system of adult mice. J Neurosci 2009; 29: 9683-99.
118. Ponimaskin EG, Profirovic J, Vaiskunaite R, Richter DW, Voyno-Yasenetskaya TA. 5-Hydroxytryptamine 4(a) receptor is coupled to the Galpha subunit of heterotrimeric G13 protein. J Biol Chem 2002; 277: 20812-9.
119. Kvachnina E, Liu G, Dityatev A, et al. 5-HT7 receptor is coupled to G alpha subunits of heterotrimeric G12-protein to regulate gene transcription and neuronal morphology. J Neurosci 2005; 25: 7821-30.
120. Ansanay H, Dumuis A, Sebben M, Bockaert J, Fagni L. cAMPdependent, long-lasting inhibition of a K+ current in mammalian neurons. Proc Natl Acad Sci USA 1995; 92: 6635-9.
121. Bockaert J, Fagni L, Dumuis A, Marin P. GPCR interacting proteins (GIP). Pharmacol Ther 2004; 103: 203-21.
122. Maillet M, Robert SJ, Cacquevel M, et al. Crosstalk between Rap1 and Rac regulates secretion of sAPPalpha. Nat Cell Biol 2003; 5: 633-9.
123. Barthet G, Framery B, Gaven F, et al. 5-hydroxytryptamine 4 receptor activation of the extracellular signal-regulated kinase pathway depends on Src activation but not on G protein or betaarrestin signaling. Mol Biol Cell 2007; 18: 1979-91.
124. Grailhe R, Waeber C, Dulawa SC, et al. Increased exploratory activity and altered response to LSD in mice lacking the 5-HT(5A) receptor. Neuron 1999; 22: 581-91.
125. Woolley ML, Marsden CA, Fone KC. 5-ht6 receptors. Curr Drug Targets CNS Neurol Disord 2004; 3: 59-79.
126. Svenningsson P, Tzavara ET, Qi H, et al. Biochemical and behavioral evidence for antidepressant-like effects of 5-HT6 receptor stimulation. J Neurosci 2007; 27: 4201-9.
127. Johnson CN, Ahmed M, Miller ND. 5-HT6 receptor antagonists: prospects for the treatment of cognitive disorders including dementia. Curr Opin Drug Discov Devel 2008; 11: 642-54.
128. Bard JA, Zgombick J, Adham N, Vaysse P, Branchek TA, Weinshank RL. Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. J Biol Chem 1993; 268: 23422-6.
129. Ruat M, Traiffort E, Leurs R, et al. Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation. Proc Natl Acad Sci USA 1993; 90: 8547-51.
130. Thomas DR, Hagan JJ. 5-HT7 receptors. Curr Drug Targets CNS Neurol Disord 2004; 3: 81-90.
131. Hedlund PB, Sutcliffe JG. Functional, molecular and pharmacological advances in 5-HT7 receptor research. Trends Pharmacol Sci 2004; 25: 481-6.
132. Doly S, Fischer J, Brisorgueil MJ, Verge D, Conrath M. Pre-and postsynaptic localization of the 5-HT7 receptor in rat dorsal spinal cord: immunocytochemical evidence. J Comp Neurol 2005; 490: 256-69.
133. Bacon WL, Beck SG. 5-Hydroxytryptamine(7) receptor activation decreases slow afterhyperpolarization amplitude in CA3 hippocampal pyramidal cells. J Pharmacol Exp Ther 2000; 294: 672-9.
134. Gill CH, Soffin EM, Hagan JJ, Davies CH. 5-HT7 receptors modulate synchronized network activity in rat hippocampus. Neuropharmacology 2002; 42: 82-92.
135. Dijk DJ, Czeisler CA. Contribution of the circadian pacemaker and the sleep homeostat to sleep propensity, sleep structure, electroencephalographic slow waves, and sleep spindle activity in humans. J Neurosci 1995; 15: 3526-38.
136. Lovenberg TW, Baron BM, de Lecea L, et al. A novel adenylyl cyclase-activating serotonin receptor (5-HT7) implicated in the regulation of mammalian circadian rhythms. Neuron 1993; 11: 449-58.
137. Ying SW, Rusak B. 5-HT7 receptors mediate serotonergic effects on light-sensitive suprachiasmatic nucleus neurons. Brain Res 1997; 755: 246-54.
138. Brenchat A, Romero L, Garcia M, et al. 5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice. Pain 2009; 141: 239-47.
139. Lin SL, Johnson-Farley NN, Lubinsky DR, Cowen DS. Coupling of neuronal 5-HT7 receptors to activation of extracellular-regulated kinase through a protein kinase A-independent pathway that can utilize Epac. J Neurochem 2003; 87: 1076-85.
140. Gurevich VV, Richardson RM, Kim CM, Hosey MM, Benovic JL. Binding of wild type and chimeric arrestins to the m2 muscarinic cholinergic receptor. J Biol Chem 1993; 268: 16879-82.
141. Freedman NJ, Ament AS, Oppermann M, Stoffel RH, Exum ST, Lefkowitz RJ. Phosphorylation and desensitization of human endothelin A and B receptors. Evidence for G protein-coupled receptor kinase specificity. J Biol Chem 1997; 272: 17734-43.
142. Reiter E, Lefkowitz RJ. GRKs and beta-arrestins: roles in receptor silencing, trafficking and signaling. Trends Endocrinol Metab 2006; 17: 159-65.
143. Oakley RH, Laporte SA, Holt JA, Barak LS, Caron MG. Molecular determinants underlying the formation of stable intracellular G protein-coupled receptor-beta-arrestin complexes after receptor endocytosis*. J Biol Chem 2001; 276: 19452-60.
144. Lefkowitz RJ, Shenoy SK. Transduction of receptor signals by beta-arrestins. Science 2005; 308: 512-7.
145. Barthet G, Gaven F, Framery B, et al. Uncoupling and endocytosis of 5-hydroxytryptamine 4 receptors. Distinct molecular events with different GRK2 requirements. J Biol Chem 2005; 280: 27924-34.
146. Gray JA, Sheffler DJ, Bhatnagar A, et al. Cell-type specific effects of endocytosis inhibitors on 5-hydroxytryptamine(2A) receptor desensitization and resensitization reveal an arrestin-, GRK2-, and GRK5-independent mode of regulation in human embryonic kidney 293 cells. Mol Pharmacol 2001; 60: 1020-30.
147. Bhatnagar A, Sheffler DJ, Kroeze WK, Compton-Toth B, Roth BL. Caveolin-1 interacts with 5-HT2A serotonin receptors and profoundly modulates the signaling of selected Galphaq-coupled protein receptors. J Biol Chem 2004; 279: 34614-23.
148. Gray JA, Bhatnagar A, Gurevich VV, Roth BL. The interaction of a constitutively active arrestin with the arrestin-insensitive 5-HT(2A) receptor induces agonist-independent internalization. Mol Pharmacol 2003; 63: 961-72.
149. Bhattacharya A, Sankar S, Panicker MM. Differences in the Cterminus contribute to variations in trafficking between rat and human 5-HT(2A) receptor isoforms: identification of a primatespecific tripeptide ASK motif that confers GRK-2 and beta arrestin-2 interactions. J Neurochem 2010; 112: 723-32.
150. Schmid CL, Raehal KM, Bohn LM. Agonist-directed signaling of the serotonin 2A receptor depends on beta-arrestin-2 interactions in vivo. Proc Natl Acad Sci USA 2008; 105: 1079-84.
151. Marion S, Oakley RH, Kim KM, Caron MG, Barak LS. A betaarrestin binding determinant common to the second intracellular loops of rhodopsin family G protein-coupled receptors. J Biol Chem 2006; 281: 2932-8.
152. Luttrell LM, Ferguson SS, Daaka Y, et al. Beta-arrestin-dependent formation of beta2 adrenergic receptor-Src protein kinase complexes. Science 1999; 283: 655-61.
153. Morrison DK, Davis RJ. Regulation of MAP kinase signaling modules by scaffold proteins in mammals. Annu Rev Cell Dev Biol 2003; 19: 91-118.
154. Xiao K, McClatchy DB, Shukla AK, et al. Functional specialization of beta-arrestin interactions revealed by proteomic analysis. Proc Natl Acad Sci USA 2007; 104: 12011-6.
155. Barthet G, Carrat G, Cassier E, et al. Beta-arrestin1 phosphorylation by GRK5 regulates G protein-independent 5-HT4 receptor signalling. EMBO J 2009; 28: 2706-18.
156. Nourry C, Grant SG, Borg JP. PDZ domain proteins: plug and play! Sci STKE 2003; 2003: RE7.
157. Becamel C, Figge A, Poliak S, et al. Interaction of serotonin 5-hydroxytryptamine type 2C receptors with PDZ10 of the multi-PDZ domain protein MUPP1. J Biol Chem 2001; 276: 12974-82.
158. Parker LL, Backstrom JR, Sanders-Bush E, Shieh BH. Agonistinduced phosphorylation of the serotonin 5-HT2C receptor regulates its interaction with multiple PDZ protein 1. J Biol Chem 2003; 278: 21576-83.
159. Xiao H, Hapiak VM, Smith KA, et al. SER-1, a Caenorhabditis elegans 5-HT2-like receptor, and a multi-PDZ domain containing protein (MPZ-1) interact in vulval muscle to facilitate serotoninstimulated egg-laying. Dev Biol 2006; 298: 379-91.
160. Kajii Y, Muraoka S, Hiraoka S, Fujiyama K, Umino A, Nishikawa T. A developmentally regulated and psychostimulant-inducible novel rat gene mrt1 encoding PDZ-PX proteins isolated in the neocortex. Mol Psychiatry 2003; 8: 434-44.
161. Compan V, Zhou M, Grailhe R, et al. Attenuated response to stress and novelty and hypersensitivity to seizures in 5-HT4 receptor knock-out mice. J Neurosci 2004; 24: 412-9.
162. Svenningsson P, Chergui K, Rachleff I, et al. Alterations in 5-HT1B receptor function by p11 in depression-like states. Science 2006; 311: 77-80.
163. Warner-Schmidt JL, Flajolet M, Maller A, et al. Role of p11 in cellular and behavioral effects of 5-HT4 receptor stimulation. J Neurosci 2009; 29: 1937-46.
164. Gerke V, Moss SE. Annexins: from structure to function. Physiol Rev 2002; 82: 331-71.
165. van de Graaf SF, Hoenderop JG, Bindels RJ. Regulation of TRPV5 and TRPV6 by associated proteins. Am J Physiol Renal Physiol 2006; 290: F1295-302.
166. + channel, TASK-1. EMBO J 2002; 21: 4439-48.
167. Poon WY, Malik-Hall M, Wood JN, Okuse K. Identification of binding domains in the sodium channel Na(V)1.8 intracellular Nterminal region and annexin II light chain p11. FEBS Lett 2004; 558: 114-8.
168. + Currents in Pulmonary Artery Smooth Muscle Cells. Role of 5-HT2A Receptors, Caveolin-1, and KV1.5 Channel Internalization. Circ Res 2006; 98: 931-8.
169. Sheffler DJ, Kroeze WK, Garcia BG, et al. p90 ribosomal S6 kinase 2 exerts a tonic brake on G protein-coupled receptor signaling. Proc Natl Acad Sci USA 2006; 103: 4717-22.
170. Thomas GM, Rumbaugh GR, Harrar DB, Huganir RL. Ribosomal S6 kinase 2 interacts with and phosphorylates PDZ domaincontaining proteins and regulates AMPA receptor transmission. Proc Natl Acad Sci USA 2005; 102: 15006-11.
171. Ji SP, Zhang Y, Van Cleemput J, et al. Disruption of PTEN coupling with 5-HT2C receptors suppresses behavioral responses induced by drugs of abuse. Nat Med 2006; 12: 324-9.
172. Takahashi Y, Morales FC, Kreimann EL, Georgescu MM. PTEN tumor suppressor associates with NHERF proteins to attenuate PDGF receptor signaling. Embo J 2006; 25: 910-20.
173. Wu Y, Dowbenko D, Spencer S, et al. Interaction of the tumor suppressor PTEN/MMAC with a PDZ domain of MAGI3, a novel membrane-associated guanylate kinase. J Biol Chem 2000; 275: 21477-85.
174. Wu X, Hepner K, Castelino-Prabhu S, et al. Evidence for regulation of the PTEN tumor suppressor by a membrane-localized multi-PDZ domain containing scaffold protein MAGI-2. Proc Natl Acad Sci USA 2000; 97: 4233-8.
175. Turner JH, Raymond JR. Interaction of calmodulin with the serotonin 5-hydroxytryptamine2A receptor. A putative regulator of G protein coupling and receptor phosphorylation by protein kinase C. J Biol Chem 2005; 280: 30741-50.
176. Turner JH, Gelasco AK, Raymond JR. Calmodulin interacts with the third intracellular loop of the serotonin 5-hydroxytryptamine1A receptor at two distinct sites: putative role in receptor phosphorylation by protein kinase C. J Biol Chem 2004; 279: 17027-37.
177. Robertson DN, Johnson MS, Moggach LO, Holland PJ, Lutz EM, Mitchell R. Selective interaction of ARF1 with the carboxyterminal tail domain of the 5-HT2A receptor. Mol Pharmacol 2003; 64: 1239-50.
178. Johnson MS, Robertson DN, Holland PJ, Lutz EM, Mitchell R. Role of the conserved NPxxY motif of the 5-HT(2A) receptor in determining selective interaction with isoforms of ADPRibosylation Factor (ARF). Cell Signal 2006; 18: 1783-800.
179. Inagaki N, Chihara K, Arimura N, et al. CRMP-2 induces axons in cultured hippocampal neurons. Nat Neurosci 2001; 4: 781-2.
180. Ward RJ, Jenkins L, Milligan G. Selectivity and functional consequences of interactions of family A G protein-coupled receptors with neurochondrin and periplakin. J Neurochem 2009; 109: 182-92.
181. Ohoka Y, Hirotani M, Sugimoto H, Fujioka S, Furuyama T, Inagaki S. Semaphorin 4C, a transmembrane semaphorin, associates with a neurite-outgrowth-related protein, SFAP75. Biochem Biophys Res Commun 2001; 280: 237-43.
182. Wang H, Westin L, Nong Y, et al. Norbin is an endogenous regulator of metabotropic glutamate receptor 5 signaling. Science 2009; 326: 1554-7.
183. Bonifacino JS, Glick BS. The mechanisms of vesicle budding and fusion. Cell 2004; 116: 153-66.
184. Xia Z, Hufeisen SJ, Gray JA, Roth BL. The PDZ-binding domain is essential for the dendritic targeting of 5-HT2A serotonin receptors in cortical pyramidal neurons in vitro. Neuroscience 2003; 122: 907-20.
185. Abbas AI, Yadav PN, Yao WD, Arbuckle MI, Grant SG, Caron MG, et al. PSD-95 is essential for hallucinogen and atypical antipsychotic drug actions at serotonin receptors. J Neurosci 2009; 29: 7124-36.
186. Weinman EJ, Hall RA, Friedman PA, Liu-Chen LY, Shenolikar S. The association of NHERF adaptor proteins with g protein-coupled receptors and receptor tyrosine kinases. Annu Rev Physiol 2006; 68: 491-505.
187. Xia Z, Gray JA, Compton-Toth BA, Roth BL. A direct interaction of PSD95 with 5-HT2A serotonin receptors regulates receptor trafficking and signal transduction. J Biol Chem 2003; 278: 21901-8.
188. Gavarini S, Becamel C, Altier C, Lory P, Poncet J, Wijnholds J, et al. Opposite Effects of PSD-95 and MPP3 PDZ Proteins on Serotonin 5-Hydroxytryptamine2C Receptor Desensitization and Membrane Stability. Mol Biol Cell 2006; 17: 4619-31.
189. Hu LA, Tang Y, Miller WE, Cong M, Lau AG, Lefkowitz RJ, et al. beta 1-adrenergic receptor association with PSD-95. Inhibition of receptor internalization and facilitation of beta 1-adrenergic receptor interaction with N-methyl-D-aspartate receptors. J Biol Chem 2000; 275: 38659-66.
190. Xu J, Paquet M, Lau AG, Wood JD, Ross CA, Hall RA. beta 1-adrenergic receptor association with the synaptic scaffolding protein membrane-associated guanylate kinase inverted-2 (MAGI-2). Differential regulation of receptor internalization by MAGI-2 and PSD-95. J Biol Chem 2001; 276: 41310-7.
191. Joubert L, Hanson B, Barthet G, Sebben M, Claeysen S, Hong W, et al. New sorting nexin (SNX27) and NHERF specifically interact with the 5-HT4a receptor splice variant: roles in receptor targeting. J Cell Sci 2004; 117: 5367-79.
192. Allen JA, Yadav PN, Roth BL. Insights into the regulation of 5-HT2A serotonin receptors by scaffolding proteins and kinases. Neuropharmacology 2008; 55: 961-8.
193. Strachan RT, Sheffler DJ, Willard B, Kinter M, Kiselar JG, Roth BL. Ribosomal S6 kinase 2 directly phosphorylates the 5-hydroxytryptamine 2A (5-HT2A) serotonin receptor, thereby modulating 5-HT2A signaling. J Biol Chem 2009; 284: 5557-73.
194. Strachan RT, Allen JA, Sheffler DJ, Roth BL. P90 Ribosomal S6 Kinase 2, a Novel Gpcr Kinase, Is Required for Growth Factor-Mediated Attenuation of Gpcr Signaling. Biochemistry 2010; 49: 2657-71.
195. Strachan RT, Sciaky N, Cronan MR, Kroeze WK, Roth BL. Genetic deletion of p90 ribosomal s6 kinase 2 alters patterns of 5-hydroxytryptamine2a serotonin receptor functional selectivity. Mol Pharmacol 2010; 77: 327-38.
196. Backstrom JR, Price RD, Reasoner DT, Sanders-Bush E. Deletion of the serotonin 5-HT2C receptor PDZ recognition motif prevents receptor phosphorylation and delays resensitization of receptor responses. J Biol Chem 2000; 275: 23620-6.
197. Esposito E. Serotonin-dopamine interaction as a focus of novel antidepressant drugs. Curr Drug Targets 2006; 7: 177-85.
198. Giorgetti M, Tecott LH. Contributions of 5-HT(2C) receptors to multiple actions of central serotonin systems. Eur J Pharmacol 2004; 488: 1-9.
199. Wu N, Hanson SM, Francis DJ, Vishnivetskiy SA, Thibonnier M, Klug CS, et al. Arrestin binding to calmodulin: a direct interaction between two ubiquitous signaling proteins. J Mol Biol 2006; 364: 955-63.
200. Geyer MA, Ellenbroek B. Animal behavior models of the mechanisms underlying antipsychotic atypicality. Prog Neuropsychopharmacol Biol Psychiatry 2003; 27: 1071-9.
201. Linn GS, Javitt DC. Phencyclidine (PCP)-induced deficits of prepulse inhibition in monkeys. Neuroreport 2001; 12: 117-20.
202. Bubar MJ, Cunningham KA. Prospects for serotonin 5-HT2R pharmacotherapy in psychostimulant abuse. Prog Brain Res 2008; 172: 319-46.
203. Shirley RL, Walter NA, Reilly MT, Fehr C, Buck KJ. Mpdz is a quantitative trait gene for drug withdrawal seizures. Nat Neurosci 2004; 7: 699-700.
204. Balasubramanian S, Fam SR, Hall RA. GABAB receptor association with the PDZ scaffold Mupp1 alters receptor stability and function. J Biol Chem 2007; 282: 4162-71.
205. El Yacoubi M, Bouali S, Popa D, Naudon L, Leroux-Nicollet I, Hamon M, et al. Behavioral, neurochemical, and electrophysiological characterization of a genetic mouse model of depression. Proc Natl Acad Sci USA 2003; 100: 6227-32.
206. Zhang X, Andren PE, Greengard P, Svenningsson P. Evidence for a role of the 5-HT1B receptor and its adaptor protein, p11, in LDOPA treatment of an animal model of Parkinsonism. Proc Natl Acad Sci USA 2008; 105: 2163-8.
207. Sun HS, Doucette TA, Liu Y, Fang Y, Teves L, Aarts M, et al. Effectiveness of PSD95 inhibitors in permanent and transient focal ischemia in the rat. Stroke 2008; 39: 2544-53.
208. Aarts M, Liu Y, Liu L, Besshoh S, Arundine M, Gurd JW, et al. Treatment of ischemic brain damage by perturbing NMDA receptor-PSD-95 protein interactions. Science 2002; 298: 846-50.
209. Liu XJ, Gingrich JR, Vargas-Caballero M, Dong YN, Sengar A, Beggs S, et al. Treatment of inflammatory and neuropathic pain by uncoupling Src from the NMDA receptor complex. Nat Med 2008; 14: 1325-32.
210. Wells JA, McClendon CL. Reaching for high-hanging fruit in drug discovery at protein-protein interfaces. Nature 2007; 450: 1001-9.