GABA B receptors-associated proteins: Potential drug targets in neurological disorders?

Current Drug Targets

Volumn 13, Issue 1, 2012, Pages 129-144

  Luján, Rafael ^a   Ciruela, Francisco ^b  

^a UNIVERSITY OF CASTILLA LA MANCHA   (Spain)

^b UNIVERSITY OF BARCELONA   (Spain)

Author keywords

Associated proteins; GABA B1; GABA B2; Ion channels; Scaffolding

Indexed keywords

2,6 DI TERT BUTYL 4 (3 HYDROXY 2,2 DIMETHYLPROPYL)PHENOL; 3 [1 [3 [(CYCLOHEXYLMETHYL)HYDROXYPHOSPHINYL] 2 HYDROXYPROPYLAMINO]ETHYL]BENZOIC ACID; 3 [1 [[2 HYDROXY 3 [HYDROXY(4 METHOXYBENZYL)PHOSPHINYL]PROPYL]AMINO]ETHYL]BENZOIC ACID; 3 AMINOPROPANEPHOSPHINIC ACID; 3 AMINOPROPYL(DIETHOXYMETHYL)PHOSPHINIC ACID; 3 AMINOPROPYL(DIFLUOROMETHYL)PHOSPHINIC ACID; 3 AMINOPROPYL(METHYL)PHOSPHINIC ACID; 3 AMINOPROPYLBUTYLPHOSPHINIC ACID; 4 AMINOBUTYRIC ACID B RECEPTOR; 4 AMINOBUTYRIC ACID B RECEPTOR BLOCKING AGENT; 4 AMINOBUTYRIC ACID B RECEPTOR STIMULATING AGENT; 5,5 DIMETHYL 2 MORPHOLINEACETIC ACID; [3 (3,4 DICHLOROBENZYLAMINO)PROPYL](DIETHOXYMETHYL)PHOSPHINIC ACID; BACLOFEN; BENZYL[3 [[1 (3,4 DICHLOROPHENYL)ETHYL]AMINO] 2 HYDROXYPROPYL]PHOSPHINIC ACID; CGP 36216; CGP 44532; CGP 44533; CGP 51176; CGP 54626A; CGP 56999A; CGP 61334; CGP 76290A; F 551; FENDILINE; ION CHANNEL; N,N' DICYCLOPENTYL 2 METHYLTHIO 5 NITRO 4,6 PYRIMIDINEDIAMINE; PHACLOFEN; SACLOFEN; UNCLASSIFIED DRUG; UNINDEXED DRUG; G PROTEIN COUPLED RECEPTOR; GABAERGIC RECEPTOR AFFECTING AGENT; HETEROTRIMERIC GUANINE NUCLEOTIDE BINDING PROTEIN;

BLOOD BRAIN BARRIER; CARBOXY TERMINAL SEQUENCE; CONFUSION; CONSTIPATION; DIZZINESS; DROWSINESS; DRUG RECEPTOR BINDING; DRUG TARGETING; FATIGUE; HEADACHE; HUMAN; HYPOTENSION; INSOMNIA; MEMBRANE TRANSPORT; MUSCLE WEAKNESS; NAUSEA; NEUROLOGIC DISEASE; NEUROMODULATION; NEUROTRANSMISSION; RESPIRATION DEPRESSION; REVIEW; SEDATION; SIDE EFFECT; URINARY FREQUENCY; ANIMAL; DRUG DELIVERY SYSTEM; DRUG EFFECT; METABOLISM; METHODOLOGY; PHYSIOLOGY; SIGNAL TRANSDUCTION;

ANIMALS; DRUG DELIVERY SYSTEMS; GABA AGENTS; HETEROTRIMERIC GTP-BINDING PROTEINS; HUMANS; NERVOUS SYSTEM DISEASES; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, GABA-B; SIGNAL TRANSDUCTION;

EID: 84855839174     PISSN: 13894501     EISSN: 18735592     Source Type: Journal    
DOI: 10.2174/138945012798868425     Document Type: Review

References (191)

1. Awapara J, Landua AJ, Fuerst R, Seale B. Free gammaaminobutyric acid in brain. J Biol Chem 1950; 187 (1): 35-9.
2. Macdonald RL, Olsen RW. GABAA receptor channels. Annu Rev Neurosci 1994; 17: 569-602.
3. Misgeld U, Bijak M, Jarolimek W. A physiological role for GABAB receptors and the effects of baclofen in the mammalian central nervous system. Prog Neurobiol 1995; 46 (4): 423-62.
4. Mott DD, Lewis DV. The pharmacology and function of central GABAB receptors. Int Rev Neurobiol 1994; 36: 97-223.
5. Kaupmann K, Schuler V, Mosbacher J, et al. Human gammaaminobutyric acid type B receptors are differentially expressed and regulate inwardly rectifying K+ channels. Proc Natl Acad Sci U S A 1998; 95 (25): 14991-6.
6. Schuler V, Luscher C, Blanchet C, et al. Epilepsy, hyperalgesia, impaired memory, and loss of pre-and postsynaptic GABA(B) responses in mice lacking GABA(B(1). Neuron 2001; 31 (1): 47-58.
7. Prosser HM, Gill CH, Hirst WD, et al. Epileptogenesis and enhanced prepulse inhibition in GABA(B1)-deficient mice. Mol Cell Neurosci 2001; 17 (6): 1059-70.
8. Mombereau C, Kaupmann K, Gassmann M, Bettler B, van der Putten H, Cryan JF. Altered anxiety and depression-related behaviour in mice lacking GABAB(2) receptor subunits. Neuroreport 2005; 16 (3): 307-10.
9. Bettler B, Kaupmann K, Mosbacher J, Gassmann M. Molecular structure and physiological functions of GABA(B) receptors. Physiol Rev 2004; 84 (3): 835-67.
10. Bowery NG, Bettler B, Froestl W, et al. International Union of Pharmacology. XXXIII. Mammalian gamma-aminobutyric acid(B) receptors: structure and function. Pharmacol Rev 2002; 54 (2): 247-64.
11. Kaupmann K, Huggel K, Heid J, et al. Expression cloning of GABA(B) receptors uncovers similarity to metabotropic glutamate receptors. Nature 1997; 386 (6622): 239-46.
12. Bowery NG, Doble A, Hill DR, et al. Bicuculline-insensitive GABA receptors on peripheral autonomic nerve terminals. Eur J Pharmacol 1981; 71 (1): 53-70.
13. Brauner-Osborne H, Wellendorph P, Jensen AA. Structure, pharmacology and therapeutic prospects of family C G-protein coupled receptors. Curr Drug Targets 2007; 8 (1): 169-84.
14. Knight AR, Bowery NG. The pharmacology of adenylyl cyclase modulation by GABAB receptors in rat brain slices. Neuropharmacology 1996; 35 (6): 703-12.
15. Pin JP, Kniazeff J, Binet V, et al. Activation mechanism of the heterodimeric GABA(B) receptor. Biochem Pharmacol 2004; 68 (8): 1565-72.
16. Bettler B, Tiao JY. Molecular diversity, trafficking and subcellular localization of GABAB receptors. Pharmacol Ther 2006; 110 (3): 533-43.
17. Pin JP, Neubig R, Bouvier M, et al. International Union of Basic and Clinical Pharmacology. LXVII. Recommendations for the recognition and nomenclature of G protein-coupled receptor heteromultimers. Pharmacol Rev 2007; 59 (1): 5-13.
18. Margeta-Mitrovic M, Jan YN, Jan LY. A trafficking checkpoint controls GABA(B) receptor heterodimerization. Neuron 2000; 27 (1): 97-106.
19. Calver AR, Robbins MJ, Cosio C, et al. The C-terminal domains of the GABA(b) receptor subunits mediate intracellular trafficking but are not required for receptor signaling. J Neurosci 2001; 21 (4): 1203-10.
20. Pagano A, Rovelli G, Mosbacher J, et al. C-terminal interaction is essential for surface trafficking but not for heteromeric assembly of GABA(b) receptors. J Neurosci 2001; 21 (4): 1189-202.
21. Galvez T, Duthey B, Kniazeff J, et al. Allosteric interactions between GB1 and GB2 subunits are required for optimal GABA(B) receptor function. EMBO J 2001; 20 (9): 2152-9.
22. Binet V, Brajon C, Le Corre L, Acher F, Pin JP, Prezeau L. The heptahelical domain of GABA(B2) is activated directly by CGP7930, a positive allosteric modulator of the GABA(B) receptor. J Biol Chem 2004; 279 (28): 29085-91.
23. Lujan R, Ciruela F. In: Molecular aspects of G protein-coupled receptors: Interacting proteins and function. Ciruela and Lujan, Ed. Hauppauge, New York, USA: Nova Science Publishers, Inc. 2007; pp 239-262.
24. Couve A, Calver AR, Fairfax B, Moss SJ, Pangalos MN. Unravelling the unusual signalling properties of the GABA(B) receptor. Biochem Pharmacol 2004; 68 (8): 1527-36.
25. Bowery NG, Brown DA. The cloning of GABA(B) receptors. Nature 1997; 386 (6622): 223-4.
26. Isomoto S, Kaibara M, Sakurai-Yamashita Y, et al. Cloning and tissue distribution of novel splice variants of the rat GABAB receptor. Biochem Biophys Res Commun 1998; 253 (1): 10-5.
27. Pfaff T, Malitschek B, Kaupmann K, et al. Alternative splicing generates a novel isoform of the rat metabotropic GABA(B)R1 receptor. Eur J Neurosci 1999; 11 (8): 2874-82.
28. Schwarz DA, Barry G, Eliasof SD, Petroski RE, Conlon PJ, Maki RA. Characterization of gamma-aminobutyric acid receptor GABAB(1e), a GABAB(1) splice variant encoding a truncated receptor. J Biol Chem 2000; 275 (41): 32174-81.
29. Lee C, Mayfield RD, Harris RA. Intron 4 containing novel GABAB1 isoforms impair GABAB receptor function. PLoS One 2010; 5 (11): e14044.
30. Billinton A, Ige AO, Bolam JP, White JH, Marshall FH, Emson PC. Advances in the molecular understanding of GABA(B) receptors. Trends Neurosci 2001; 24 (5): 277-82.
31. Billinton A, Upton N, Bowery NG. GABA(B) receptor isoforms GBR1a and GBR1b, appear to be associated with pre-and postsynaptic elements respectively in rat and human cerebellum. Br J Pharmacol 1999; 126 (6): 1387-92.
32. Tiao JY, Bradaia A, Biermann B, et al. The sushi domains of secreted GABA(B1) isoforms selectively impair GABA(B) heteroreceptor function. J Biol Chem 2008; 283 (45): 31005-11.
33. Martin SC, Russek SJ, Farb DH. Human GABA(B)R genomic structure: evidence for splice variants in GABA(B)R1 but not GABA(B)R2. Gene 2001; 278 (1-2): 63-79.
34. Bowery NG, Hill DR, Hudson AL, et al. (-)Baclofen decreases neurotransmitter release in the mammalian CNS by an action at a novel GABA receptor. Nature 1980; 283 (5742): 92-4.
35. Bowery NG, Doble A, Hill DR, et al. Bicuculline-insensitive GABA receptors on peripheral autonomic nerve terminals. Eur J Pharmacol 1981; 71 (1): 53-70.
36. Vacher CM, Bettler B. GABA(B) receptors as potential therapeutic targets. Curr Drug Targets CNS Neurol Disord 2003; 2 (4): 248-59.
37. Bettler B, Kaupmann K, Mosbacher J, Gassmann M. Molecular structure and physiological functions of GABA(B) receptors. Physiol Rev 2004; 84 (3): 835-67.
38. Ong J, Kerr DI. Clinical potential of GABAB receptor modulators. CNS Drug Rev 2005; 11 (3): 317-34.
39. Bowery NG. GABAB receptor: a site of therapeutic benefit. Curr Opin Pharmacol 2006; 6 (1): 37-43.
40. Asano T, Ui M, Ogasawara N. Prevention of the agonist binding to gamma-aminobutyric acid B receptors by guanine nucleotides and islet-activating protein, pertussis toxin, in bovine cerebral cortex. Possible coupling of the toxin-sensitive GTP-binding proteins to receptors. J Biol Chem 1985; 260 (23): 12653-8.
41. Morishita R, Kato K, Asano T. GABAB receptors couple to G proteins Go, Go* and Gi1 but not to Gi2. FEBS Lett 1990; 271 (1-2): 231-5.
42. Cui LN, Coderre E, Renaud LP. GABA(B) presynaptically modulates suprachiasmatic input to hypothalamic paraventricular magnocellular neurons. Am J Physiol Regul Integr Comp Physiol 2000; 278 (5): R1210-6.
43. Margeta-Mitrovic M, Jan YN, Jan LY. Ligand-induced signal transduction within heterodimeric GABA(B) receptor. Proc Natl Acad Sci U S A 2001; 98 (25): 14643-8.
44. Harayama N, Shibuya I, Tanaka K, Kabashima N, Ueta Y, Yamashita H. Inhibition of N-and P/Q-type calcium channels by postsynaptic GABAB receptor activation in rat supraoptic neurones. J Physiol 1998; 509 (Pt 2): 371-83.
45. Luscher C, Jan LY, Stoffel M, Malenka RC, Nicoll RA. G proteincoupled inwardly rectifying K+ channels (GIRKs) mediate postsynaptic but not presynaptic transmitter actions in hippocampal neurons. Neuron 1997; 19 (3): 687-95.
46. Harrison NL. On the presynaptic action of baclofen at inhibitory synapses between cultured rat hippocampal neurones. J Physiol 1990; 422: 433-46.
47. Catterall WA, Perez-Reyes E, Snutch TP, Striessnig J. International Union of Pharmacology. XLVIII. Nomenclature and structurefunction relationships of voltage-gated calcium channels. Pharmacol Rev 2005; 57 (4): 411-25.
48. Wu LG, Saggau P. Presynaptic inhibition of elicited neurotransmitter release. Trends Neurosci 1997; 20 (5): 204-12.
49. Xu J, Wojcik WJ. Gamma aminobutyric acid B receptor-mediated inhibition of adenylate cyclase in cultured cerebellar granule cells: blockade by islet-activating protein. J Pharmacol Exp Ther 1986; 239 (2): 568-73.
50. Enna SJ. Pharmacology of GABA and Glycine Neurotransmission, Springer-Verlag 2000, Berlin.
51. Lehmann A. GABAB receptors as drug targets to treat gastroesophageal reflux disease. Pharmacol Ther 2009; 122 (3): 239-45.
52. Meza G. Gaba as an afferent neurotransmitter in the vestibular sensory periphery of vertebrates. Neurobiology (Bp) 1998; 6 (1): 109-25.
53. Ong J, Kerr DI. GABA-receptors in peripheral tissues. Life Sci 1990; 46 (21): 1489-501.
54. Jones KA, Borowsky B, Tamm JA, et al. GABA(B) receptors function as a heteromeric assembly of the subunits GABA(B)R1 and GABA(B)R2. Nature 1998; 396 (6712): 674-9.
55. Munoz A, Huntsman MM, Jones EG. GABA(B) receptor gene expression in monkey thalamus. J Comp Neurol 1998; 394 (1): 118-26.
56. Durkin MM, Gunwaldsen CA, Borowsky B, Jones KA, Branchek TA. An in situ hybridization study of the distribution of the GABA(B2) protein mRNA in the rat CNS. Brain Res Mol Brain Res 1999; 71 (2): 185-200.
57. Fritschy JM, Meskenaite V, Weinmann O, Honer M, Benke D, Mohler H. GABAB-receptor splice variants GB1a and GB1b in rat brain: developmental regulation, cellular distribution and extrasynaptic localization. Eur J Neurosci 1999; 11 (3): 761-8.
58. Margeta-Mitrovic M, Mitrovic I, Riley RC, Jan LY, Basbaum AI. Immunohistochemical localization of GABA(B) receptors in the rat central nervous system. J Comp Neurol 1999; 405 (3): 299-321.
59. Ige AO, Bolam JP, Billinton A, White JH, Marshall FH, Emson PC. Cellular and sub-cellular localisation of GABA(B1) and GABA(B2) receptor proteins in the rat cerebellum. Brain Res Mol Brain Res 2000; 83 (1-2): 72-80.
60. Liang F, Hatanaka Y, Saito H, Yamamori T, Hashikawa T. Differential expression of gamma-aminobutyric acid type B receptor-1a and-1b mRNA variants in GABA and non-GABAergic neurons of the rat brain. J Comp Neurol 2000; 416 (4): 475-95.
61. Berthele A, Platzer S, Weis S, Conrad B, Tolle TR. Expression of GABA(B1) and GABA(B2) mRNA in the human brain. Neuroreport 2001; 12 (15): 3269-75.
62. Charles KJ, Evans ML, Robbins MJ, Calver AR, Leslie RA, Pangalos MN. Comparative immunohistochemical localisation of GABA(B1a), GABA(B1b) and GABA(B2) subunits in rat brain, spinal cord and dorsal root ganglion. Neuroscience 2001; 106 (3): 447-67.
63. Gonchar Y, Pang L, Malitschek B, Bettler B, Burkhalter A. Subcellular localization of GABA(B) receptor subunits in rat visual cortex. J Comp Neurol 2001; 431 (2): 182-97.
64. Kulik A, Nakadate K, Nyiri G, et al. Distinct localization of GABA(B) receptors relative to synaptic sites in the rat cerebellum and ventrobasal thalamus. Eur J Neurosci 2002; 15 (2): 291-307.
65. Lopez-Bendito G, Shigemoto R, Kulik A, Paulsen O, Fairen A, Lujan R. Expression and distribution of metabotropic GABA receptor subtypes GABABR1 and GABABR2 during rat neocortical development. Eur J Neurosci 2002; 15 (11): 1766-78.
66. Charles KJ, Calver AR, Jourdain S, Pangalos MN. Distribution of a GABAB-like receptor protein in the rat central nervous system. Brain Res 2003; 989 (2): 135-46.
67. Kulik A, Vida I, Lujan R, et al. Subcellular localization of metabotropic GABA(B) receptor subunits GABA(B1a/b) and GABA(B2) in the rat hippocampus. J Neurosci 2003; 23 (35): 11026-35.
68. Lopez-Bendito G, Shigemoto R, Kulik A, Vida I, Fairen A, Lujan R. Distribution of metabotropic GABA receptor subunits GABAB1a/b and GABAB2 in the rat hippocampus during prenatal and postnatal development. Hippocampus 2004; 14 (7): 836-48.
69. Lujan R, Shigemoto R, Kulik A, Juiz JM. Localization of the GABAB receptor 1a/b subunit relative to glutamatergic synapses in the dorsal cochlear nucleus of the rat. J Comp Neurol 2004; 475 (1): 36-46.
70. Lujan R, Shigemoto R. Localization of metabotropic GABA receptor subunits GABAB1 and GABAB2 relative to synaptic sites in the rat developing cerebellum. Eur J Neurosci 2006; 23 (6): 1479-90.
71. Vigot R, Barbieri S, Brauner-Osborne H, et al. Differential compartmentalization and distinct functions of GABAB receptor variants. Neuron 2006; 50 (4): 589-601.
72. Lujan R, Shigemoto R. Localization of metabotropic GABA receptor subunits GABAB1 and GABAB2 relative to synaptic sites in the rat developing cerebellum. Eur J Neurosci 2006; 23 (6): 1479-90.
73. Kaupmann K, Malitschek B, Schuler V, et al. GABA(B)-receptor subtypes assemble into functional heteromeric complexes. Nature 1998; 396 (6712): 683-7.
74. Zilberter Y, Kaiser KM, Sakmann B. Dendritic GABA release depresses excitatory transmission between layer 2/3 pyramidal and bitufted neurons in rat neocortex. Neuron 1999; 24 (4): 979-88.
75. Lei S, McBain CJ. GABA B receptor modulation of excitatory and inhibitory synaptic transmission onto rat CA3 hippocampal interneurons. J Physiol 2003; 546 (Pt 2): 439-53.
76. Porter JT, Nieves D. Presynaptic GABAB receptors modulate thalamic excitation of inhibitory and excitatory neurons in the mouse barrel cortex. J Neurophysiol 2004; 92 (5): 2762-70.
77. Leung LS, Peloquin P. GABA(B) receptors inhibit backpropagating dendritic spikes in hippocampal CA1 pyramidal cells in vivo. Hippocampus 2006; 16 (4): 388-407.
78. Malitschek B, Ruegg D, Heid J, et al. Developmental changes of agonist affinity at GABABR1 receptor variants in rat brain. Mol Cell Neurosci 1998; 12 (1-2): 56-64.
79. Princivalle A, Spreafico R, Bowery N, De Curtis M. Layer-specific immunocytochemical localization of GABA(B)R1a and GABA(B)R1b receptors in the rat piriform cortex. Eur J Neurosci 2000; 12 (4): 1516-20.
80. Zhang C, Bettler B, Duvoisin RM. Differential localization of GABA(B) receptors in the mouse retina. Neuroreport 1998; 9 (15): 3493-7.
81. Biermann B, Ivankova-Susankova K, Bradaia A, et al. The Sushi domains of GABAB receptors function as axonal targeting signals. J Neurosci 2010; 30 (4): 1385-94.
82. Perez-Garci E, Gassmann M, Bettler B, Larkum ME. The GABAB1b isoform mediates long-lasting inhibition of dendritic Ca2+ spikes in layer 5 somatosensory pyramidal neurons. Neuron 2006; 50 (4): 603-16.
83. Steiger JL, Bandyopadhyay S, Farb DH, Russek SJ. cAMP response element-binding protein, activating transcription factor-4, and upstream stimulatory factor differentially control hippocampal GABABR1a and GABABR1b subunit gene expression through alternative promoters. J Neurosci 2004; 24 (27): 6115-26.
84. Bowery NG, Bettler B, Froestl W, et al. International Union of Pharmacology. XXXIII. Mammalian gamma-aminobutyric acid(B) receptors: structure and function. Pharmacol Rev 2002; 54 (2): 247-64.
85. Bittiger H, Reymann N, Hall R, Kane P. CGP27492, a new potent and selective radioligand for GABAB receptors. Eur J Neurosci 1988; 16 (Suppl): 10.
86. Froestl W, Mickel SJ, von Sprecher G, Bittiger H, Olpe HR. Chemistry of new GABAB antagonists. Pharmacol Commun 1992; 2: 52-6.
87. Froestl W, Mickel SJ, Bittiger H. Potents GABAB agonists and antagonists. Curr Opin Therap Patents 1993; 3: 561-7.
88. Howson W, Mistry J, Broekman M, Hills JM. Biological activity of 3-aminopropyl (methyl) phosphinic acid, a potent and selective GABAB agonist with CNS activity. Bioorg Med Chem Lett 1993; 3: 515-8.
89. Froestl W, Mickel SJ, Hall RG, et al. Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. J Med Chem 1995; 38 (17): 3297-312.
90. Vergnes M, Boehrer A, Simler S, Bernasconi R, Marescaux C. Opposite effects of GABAB receptor antagonists on absences and convulsive seizures. Eur J Pharmacol 1997; 332 (3): 245-55.
91. Kerr DI, Ong J, Prager RH, Gynther BD, Curtis DR. Phaclofen: a peripheral and central baclofen antagonist. Brain Res 1987; 405 (1): 150-4.
92. Kerr DI, Ong J, Johnston GA, Abbenante J, Prager RH. 2-Hydroxy-saclofen: an improved antagonist at central and peripheral GABAB receptors. Neurosci Lett 1988; 92 (1): 92-6.
93. Kerr DI, Ong J, Johnston GA, Abbenante J, Prager RH. Antagonism at GABAB receptors by saclofen and related sulphonic analogues of baclofen and GABA. Neurosci Lett 1989; 107 (1-3): 239-44.
94. Kerr DIB, Ong J. GABA agonists and antagonists. Med Res Rev 1992; 12: 593.
95. Olpe HR, Karlsson G, Pozza MF, et al. CGP 35348: a centrally active blocker of GABAB receptors. Eur J Pharmacol 1990; 187 (1): 27-38.
96. Olpe HR, Steinmann MW, Ferrat T, et al. The actions of orally active GABAB receptor antagonists on GABAergic transmission in vivo and in vitro. Eur J Pharmacol 1993; 233 (2-3): 179-86.
97. Ong J, Bexis S, Marino V, Parker DA, Kerr DI, Froestl W. Comparative activities of the enantiomeric GABA(B) receptor agonists CGP 44532 and 44533 in central and peripheral tissues. Eur J Pharmacol 2001; 412 (1): 27-37.
98. Conn PJ, Christopoulos A, Lindsley CW. Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat Rev Drug Discov 2009; 8 (1): 41-54.
99. Pin JP, Prezeau L. Allosteric modulators of GABA(B) receptors: mechanism of action and therapeutic perspective. Curr Neuropharmacol 2007; 5 (3): 195-201.
100. Urwyler S, Mosbacher J, Lingenhoehl K, et al. Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethylpropyl)-phenol (CGP7930) and its aldehyde analog CGP13501. Mol Pharmacol 2001; 60 (5): 963-71.
101. Urwyler S, Pozza MF, Lingenhoehl K, et al. N, N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function. J Pharmacol Exp Ther 2003; 307 (1): 322-30.
102. Kerr DI, Ong J, Puspawati NM, Prager RH. Arylalkylamines are a novel class of positive allosteric modulators at GABA(B) receptors in rat neocortex. Eur J Pharmacol 2002; 451 (1): 69-77.
103. Kerr DIB, Ong J, Puspawati NM, Prager RH. Allosteric modulation: a new perspective in GABAB receptor pharmacology. Curr Topics Pharmacol 2004; 8: 17-29.
104. Ong J, Parker DA, Marino V, Kerr DI, Puspawati NM, Prager RH. 3-Chloro,4-methoxyfendiline is a potent GABA(B) receptor potentiator in rat neocortical slices. Eur J Pharmacol 2005; 507 (1-3): 35-42.
105. Hammerland LG, Garrett JE, Hung BC, Levinthal C, Nemeth EF. Allosteric activation of the Ca2+ receptor expressed in Xenopus laevis oocytes by NPS 467 or NPS 568. Mol Pharmacol 1998; 53 (6): 1083-8.
106. Asano T, Ogasawara N. Uncoupling of gamma-aminobutyric acid B receptors from GTP-binding proteins by N-ethylmaleimide: effect of N-ethylmaleimide on purified GTP-binding proteins. Mol Pharmacol 1986; 29 (3): 244-9.
107. Campbell V, Berrow N, Dolphin AC. GABAB receptor modulation of Ca2+ currents in rat sensory neurones by the G protein G(0): antisense oligonucleotide studies. J Physiol 1993; 470: 1-11.
108. Greif GJ, Sodickson DL, Bean BP, Neer EJ, Mende U. Altered regulation of potassium and calcium channels by GABA(B) and adenosine receptors in hippocampal neurons from mice lacking Galpha(o). J Neurophysiol 2000; 83 (2): 1010-8.
109. Hofmann KP, Scheerer P, Hildebrand PW, et al. A G proteincoupled receptor at work: the rhodopsin model. Trends Biochem Sci 2009; 34 (11): 540-52.
110. Oldham WM, Hamm HE. Structural basis of function in heterotrimeric G proteins. Q Rev Biophys 2006; 39 (2): 117-66.
111. Willars GB, Mammalian RGS proteins: multifunctional regulators of cellular signalling. Semin Cell Dev Biol 2006; 17 (3): 363-76.
112. Magalhaes AC, Dunn H, Ferguson SS. Regulation of G Protein-Coupled Receptor Activity, Trafficking and Localization by Gpcr-Interacting Proteins. Br J Pharmacol 2011; (In press).
113. Abramow-Newerly M, Roy AA, Nunn C, Chidiac P. RGS proteins have a signalling complex: interactions between RGS proteins and GPCRs, effectors, and auxiliary proteins. Cell Signal 2006; 18 (5): 579-91.
114. Ross EM, Wilkie TM. GTPase-activating proteins for heterotrimeric G proteins: regulators of G protein signaling (RGS) and RGS-like proteins. Annu Rev Biochem 2000; 69: 795-827.
115. De Vries L, Zheng B, Fischer T, Elenko E, Farquhar MG. The regulator of G protein signaling family. Annu Rev Pharmacol Toxicol 2000; 40: 235-71.
116. Siderovski DP, Willard FS. The GAPs, GEFs, and GDIs of heterotrimeric G-protein alpha subunits. Int J Biol Sci 2005; 1 (2): 51-66.
117. Kim E, Arnould T, Sellin L, et al. Interaction between RGS7 and polycystin. Proc Natl Acad Sci U S A 1999; 96 (11): 6371-6.
118. Roy AA, Lemberg KE, Chidiac P. Recruitment of RGS2 and RGS4 to the plasma membrane by G proteins and receptors reflects functional interactions. Mol Pharmacol 2003; 64 (3): 587-93.
119. Song L, De Sarno P, Jope RS. Muscarinic receptor stimulation increases regulators of G-protein signaling 2 mRNA levels through a protein kinase C-dependent mechanism. J Biol Chem 1999; 274 (42): 29689-93.
120. Schiff ML, Siderovski DP, Jordan JD, et al. Tyrosine-kinasedependent recruitment of RGS12 to the N-type calcium channel. Nature 2000; 408 (6813): 723-7.
121. Chatterjee TK, Liu Z, Fisher RA. Human RGS6 gene structure, complex alternative splicing, and role of N terminus and G protein gamma-subunit-like (GGL) domain in subcellular localization of RGS6 splice variants. J Biol Chem 2003; 278 (32): 30261-71.
122. Labouebe G, Lomazzi M, Cruz HG, et al. RGS2 modulates coupling between GABAB receptors and GIRK channels in dopamine neurons of the ventral tegmental area. Nat Neurosci 2007; 10 (12): 1559-68.
123. Kelly MJ, Lagrange AH, Wagner EJ, Ronnekleiv OK. Rapid effects of estrogen to modulate G protein-coupled receptors via activation of protein kinase A and protein kinase C pathways. Steroids 1999; 64 (1-2): 64-75.
124. Couve A, Thomas P, Calver AR, et al, Moss SJ. Cyclic AMPdependent protein kinase phosphorylation facilitates GABA(B) receptor-effector coupling. Nat Neurosci 2002; 5 (5): 415-24.
125. Balasubramanian S, Teissere JA, Raju DV, Hall RA. Heterooligomerization between GABAA and GABAB receptors regulates GABAB receptor trafficking. J Biol Chem 2004; 279 (18): 18840-50.
126. Gomez-Soler M, Ahern S, Fernandez-Dueñas V, Ciruela F. On the role of G protein-coupled receptors oligomerization. Open Biol J 2011; 4 (1): 47-53.
127. Ciruela F, Vallano A, Arnau JM, et al. G protein-coupled receptor oligomerization for what? J Recept Signal Transduct Res 2010; 30 (5): 322-30.
128. Tabata T, Kano M. GABA(B) receptor-mediated modulation of glutamate signaling in cerebellar Purkinje cells. Cerebellum 2006; 5 (2): 127-33.
129. Sullivan R, Chateauneuf A, Coulombe N, et al. Coexpression of full-length gamma-aminobutyric acid(B) (GABA(B) receptors with truncated receptors and metabotropic glutamate receptor 4 supports the GABA(B) heterodimer as the functional receptor. J Pharmacol Exp Ther 2000; 293 (2): 460-7.
130. Corti C, Aldegheri L, Somogyi P, Ferraguti F. Distribution and synaptic localisation of the metabotropic glutamate receptor 4 (mGluR4) in the rodent CNS. Neuroscience 2002; 110 (3): 403-20.
131. North A. Drug receptors and the inhibition of nerve cells. Br J Pharmacol 1989; 98: 13-28.
132. Peleg S, Varon D, Ivanina T, Dessauer CW, Dascal N. G(alpha)(i) controls the gating of the G protein-activated K(+) channel, GIRK. Neuron 2002; 33 (1): 87-99.
133. Ivanina T, Rishal I, Varon D, et al. Mapping the Gbetagammabinding sites in GIRK1 and GIRK2 subunits of the G proteinactivated K+ channel. J Biol Chem 2003; 278 (31): 29174-83.
134. Clancy SM, Fowler CE, Finley M, et al. Pertussis-toxin-sensitive Galpha subunits selectively bind to C-terminal domain of neuronal GIRK channels: evidence for a heterotrimeric G-protein-channel complex. Mol Cell Neurosci 2005; 28 (2): 375-89.
135. Nikolov EN, Ivanova-Nikolova TT. Coordination of membrane excitability through a GIRK1 signaling complex in the atria. J Biol Chem 2004; 279 (22): 23630-6.
136. Kubo Y, Adelman JP, Clapham DE, et al. International Union of Pharmacology. LIV. Nomenclature and molecular relationships of inwardly rectifying potassium channels. Pharmacol Rev 2005; 57 (4): 509-26.
137. Bichet D, Haass FA, Jan LY. Merging functional studies with structures of inward-rectifier K(+) channels. Nat Rev Neurosci 2003; 4 (12): 957-67.
138. Krapivinsky G, Gordon EA, Wickman K, Velimirovic B, Krapivinsky L, Clapham DE. The G-protein-gated atrial K+ channel IKACh is a heteromultimer of two inwardly rectifying K(+)-channel proteins. Nature 1995; 374 (6518): 135-41.
139. Kubo Y, Reuveny E, Slesinger PA, Jan YN, Jan LY. Primary structure and functional expression of a rat G-protein-coupled muscarinic potassium channel. Nature 1993; 364 (6440): 802-6.
140. Lesage F, Duprat F, Fink M, et al. Cloning provides evidence for a family of inward rectifier and G-protein coupled K+ channels in the brain. FEBS Lett 1994; 353 (1): 37-42.
141. Lesage F, Fink M, Barhanin J, Lazdunski M, Mattei MG. Assignment of human G-protein-coupled inward rectifier K+ channel homolog GIRK3 gene to chromosome 1q21-q23. Genomics 1995; 29 (3): 808-9.
142. Karschin C, Dissmann E, Stuhmer W, Karschin A. IRK(1-3) and GIRK(1-4) inwardly rectifying K+ channel mRNAs are differentially expressed in the adult rat brain. J Neurosci 1996; 16 (11): 3559-70.
143. Wickman K, Karschin C, Karschin A, Picciotto MR, Clapham DE. Brain localization and behavioral impact of the G-protein-gated K+ channel subunit GIRK4. J Neurosci 2000; 20 (15): 5608-15.
144. Koyrakh L, Lujan R, Colon J, et al. Molecular and cellular diversity of neuronal G-protein-gated potassium channels. J Neurosci 2005; 25 (49): 11468-78.
145. Marker CL, Lujan R, Loh HH, Wickman K. Spinal G-protein-gated potassium channels contribute in a dose-dependent manner to the analgesic effect of mu-and delta-but not kappa-opioids. J Neurosci 2005; 25 (14): 3551-9.
146. Ciruela F, Fernandez-Duenas V, Sahlholm K, et al. Evidence for oligomerization between GABAB receptors and GIRK channels containing the GIRK1 and GIRK3 subunits. Eur J Neurosci 2010; 32 (8): 1265-77.
147. Kulik A, Nakadate K, Hagiwara A, et al. Immunocytochemical localization of the alpha 1A subunit of the P/Q-type calcium channel in the rat cerebellum. Eur J Neurosci 2004; 19 (8): 2169-78.
148. Chalifoux JR, Carter AG. GABAB receptor modulation of voltagesensitive calcium channels in spines and dendrites. J Neurosci 2011; 31 (11): 4221-32.
149. Couve A, Kittler JT, Uren JM, et al. Association of GABA(B) receptors and members of the 14-3-3 family of signaling proteins. Mol Cell Neurosci 2001; 17 (2): 317-28.
150. Fu H, Subramanian RR, Masters SC. 14-3-3 Proteins: Structure, Function, and Regulation. Annu Rev Pharmacol Toxicol 2000; 40: 617-47.
151. Pontier SM, Lahaie N, Ginham R, et al. Coordinated action of NSF and PKC regulates GABAB receptor signaling efficacy. EMBO J 2006; 25 (12): 2698-709.
152. Kittler JT, Rostaing P, Schiavo G, et al. The subcellular distribution of GABARAP and its ability to interact with NSF suggest a role for this protein in the intracellular transport of GABA(A) receptors. Mol Cell Neurosci 2001; 18 (1): 13-25.
153. Kitano J, Kimura K, Yamazaki Y, et al. Tamalin, a PDZ domaincontaining protein, links a protein complex formation of group 1 metabotropic glutamate receptors and the guanine nucleotide exchange factor cytohesins. J Neurosci 2002; 22 (4): 1280-9.
154. Harris BZ, Lim WA. Mechanism and role of PDZ domains in signaling complex assembly. J Cell Sci 2001; 114 (Pt 18): 3219-31.
155. Kornau HC, Schenker LT, Kennedy MB, Seeburg PH. Domain interaction between NMDA receptor subunits and the postsynaptic density protein PSD-95. Science 1995; 269 (5231): 1737-40.
156. Balasubramanian S, Fam SR, Hall RA. GABAB receptor association with the PDZ scaffold Mupp1 alters receptor stability and function. J Biol Chem 2007; 282 (6): 4162-71.
157. Nehring RB, Horikawa HP, El Far O, et al. The metabotropic GABAB receptor directly interacts with the activating transcription factor 4. J Biol Chem 2000; 275 (45): 35185-91.
158. Vernon E, Meyer G, Pickard L, et al. GABA(B) receptors couple directly to the transcription factor ATF4. Mol Cell Neurosci 2001; 17 (4): 637-45.
159. White JH, McIllhinney RA, Wise A, et al. The GABAB receptor interacts directly with the related transcription factors CREB2 and ATFx. Proc Natl Acad Sci U S A 2000; 97 (25): 13967-72.
160. Heese K, Otten U, Mathivet P, Raiteri M, Marescaux C, Bernasconi R. GABA(B) receptor antagonists elevate both mRNA and protein levels of the neurotrophins nerve growth factor (NGF) and brain-derived neurotrophic factor (BDNF) but not neurotrophin-3 (NT-3) in brain and spinal cord of rats. Neuropharmacology 2000; 39 (3): 449-62.
161. Sauter K, Grampp T, Fritschy JM, et al. Subtype-selective interaction with the transcription factor CCAAT/enhancer-binding protein (C/EBP) homologous protein (CHOP) regulates cell surface expression of GABA(B) receptors. J Biol Chem 2005; 280 (39): 33566-72.
162. Oyadomari S, Araki E, Mori M. Endoplasmic reticulum stressmediated apoptosis in pancreatic beta-cells. Apoptosis 2002; 7 (4): 335-45.
163. Oyadomari S, Koizumi A, Takeda K, et al. Targeted disruption of the Chop gene delays endoplasmic reticulum stress-mediated diabetes. J Clin Invest 2002; 109 (4): 525-32.
164. Oyadomari S, Takeda K, Takiguchi M, et al. Nitric oxide-induced apoptosis in pancreatic beta cells is mediated by the endoplasmic reticulum stress pathway. Proc Natl Acad Sci U S A 2001; 98 (19): 10845-50.
165. Zinszner H, Kuroda M, Wang X, et al. CHOP is implicated in programmed cell death in response to impaired function of the endoplasmic reticulum. Genes Dev 1998; 12 (7): 982-95.
166. Tajiri S, Oyadomari S, Yano S, et al. Ischemia-induced neuronal cell death is mediated by the endoplasmic reticulum stress pathway involving CHOP. Cell Death Differ 2004; 11 (4): 403-15.
167. Schwenk J, Metz M, Zolles G, et al. Native GABA(B) receptors are heteromultimers with a family of auxiliary subunits. Nature 2010; 465 (7295): 231-5.
168. Metz M, Gassmann M, Fakler B, Schaeren-Wiemers N, Bettler B. Distribution of the auxiliary GABAB receptor subunits KCTD8, 12, 12b, and 16 in the mouse brain. J Comp Neurol 2011; 519 (8): 1435-54.
169. Couve A, Restituito S, Brandon JM, et al. Marlin-1, a novel RNAbinding protein associates with GABA receptors. J Biol Chem 2004; 279 (14): 13934-43.
170. Ginham R, Blein S, Barlow P, White J, McIlhinney RA. Interaction of "Sushi" domain of GABA-BR1a subunit with the extracellular matrix protein fibulin. FENS Abstr 2002; 1: 144-6.
171. Saghatelyan AK, Snapyan M, Gorissen S, et al. Recognition molecule associated carbohydrate inhibits postsynaptic GABA(B) receptors: a mechanism for homeostatic regulation of GABA release in perisomatic synapses. Mol Cell Neurosci 2003; 24 (2): 271-82.
172. Cryan JF, Kaupmann K. Don't worry 'B' happy!: a role for GABA(B) receptors in anxiety and depression. Trends Pharmacol Sci 2005; 26 (1): 36-43.
173. McDonald AJ, Mascagni F, Muller JF. Immunocytochemical localization of GABABR1 receptor subunits in the basolateral amygdala. Brain Res 2004; 1018 (2): 147-58.
174. Mombereau C, Kaupmann K, Froestl W, Sansig G, van der Putten H, Cryan JF. Genetic and pharmacological evidence of a role for GABA(B) receptors in the modulation of anxiety-and antidepressant-like behavior. Neuropsychopharmacology 2004; 29 (6): 1050-62.
175. Cryan JF, Kelly PH, Chaperon F, et al. Behavioral characterization of the novel GABAB receptor-positive modulator GS39783 (N, N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine): anxiolytic-like activity without side effects associated with baclofen or benzodiazepines. J Pharmacol Exp Ther 2004; 310 (3): 952-63.
176. Nakagawa Y, Sasaki A, Takashima T. The GABA(B) receptor antagonist CGP36742 improves learned helplessness in rats. Eur J Pharmacol 1999; 381 (1): 1-7.
177. Slattery DA, Desrayaud S, Cryan JF. GABAB receptor antagonistmediated antidepressant-like behavior is serotonin-dependent. J Pharmacol Exp Ther 2005; 312 (1): 290-6.
178. Erwin A, Gudesblatt M, Bethoux F, et al. Intrathecal baclofen in multiple sclerosis: too little, too late? Mult Scler 2011; 17 (5): 623-9.
179. Liu J, Wang L. Baclofen for alcohol withdrawal. Cochrane Database Syst Rev 2011; (1): CD008502.
180. Soudijn W, Van Wijngaarden I, IJzerman AP. Allosteric modulation of G protein-coupled receptors: perspectives and recent developments. Drug Discov Today 2004; 9 (17): 752-8.
181. May LT, Leach K, Sexton PM, Christopoulos A. Allosteric modulation of G protein-coupled receptors. Annu Rev Pharmacol Toxicol 2007; 47: 1-51.
182. Pagliaro L, Felding J, Audouze K, et al. Emerging classes of protein-protein interaction inhibitors and new tools for their development. Curr Opin Chem Biol 2004; 8 (4): 442-9.
183. Buchwald P. Small-molecule protein-protein interaction inhibitors: therapeutic potential in light of molecular size, chemical space, and ligand binding efficiency considerations. IUBMB Life 2010; 62 (10): 724-31.
184. Arkin MR, Wells JA. Small-molecule inhibitors of protein-protein interactions: progressing towards the dream. Nat Rev Drug Discov 2004; 3 (4): 301-17.
185. Sugaya N, Ikeda K. Assessing the druggability of protein-protein interactions by a supervised machine-learning method. BMC Bioinformatics 2009; 10: 263.
186. Wilson AJ. Inhibition of protein-protein interactions using designed molecules. Chem Soc Rev 2009; 38 (12): 3289-300.
187. Fujii N, Haresco JJ, Novak KA, Stokoe D, Kuntz ID, Guy RK. A selective irreversible inhibitor targeting a PDZ protein interaction domain. J Am Chem Soc 2003; 125 (40): 12074-5.
188. Fujii N, Haresco JJ, Novak KA, et al. Rational design of a nonpeptide general chemical scaffold for reversible inhibition of PDZ domain interactions. Bioorg Med Chem Lett 2007; 17 (2): 549-52.
189. Thorsen TS, Madsen KL, Rebola N, et al. Identification of a smallmolecule inhibitor of the PICK1 PDZ domain that inhibits hippocampal LTP and LTD. Proc Natl Acad Sci U S A 2010; 107 (1): 413-8.
190. Zhang W, Penmatsa H, Ren A, et al. Functional regulation of cystic fibrosis transmembrane conductance regulator-containing macromolecular complexes: a small-molecule inhibitor approach. Biochem J 2011; 435 (2): 451-62.
191. Robbins MJ, Calver AR, Filippov AK, et al. GABA(B2) is essential for g-protein coupling of the GABA(B) receptor heterodimer. J Neurosci 2001; 21 (20): 8043-52.