Receptor metabotrópico de glutamato 5
O receptor metabotrópico de glutamato 5 é uma proteína que em seres humanos é codificada pelo gene GRM5.[1][2][3] Os receptores metabotrópicos de glutamato são uma família de receptores acoplados à proteína G.
Antagonistas
- Mavoglurant
- Remeglurant
- LY-344,545
Referências
Bibliografia
- Minakami R, Katsuki F, Sugiyama H (1993). «A variant of metabotropic glutamate receptor subtype 5: an evolutionally conserved insertion with no termination codon.». Biochem. Biophys. Res. Commun. 194 (2): 622–7. PMID 7688218. doi:10.1006/bbrc.1993.1866
- Daggett LP, Sacaan AI, Akong M; et al. (1996). «Molecular and functional characterization of recombinant human metabotropic glutamate receptor subtype 5.». Neuropharmacology. 34 (8): 871–86. PMID 8532169. doi:10.1016/0028-3908(95)00085-K
- Brakeman PR, Lanahan AA, O'Brien R; et al. (1997). «Homer: a protein that selectively binds metabotropic glutamate receptors.». Nature. 386 (6622): 284–8. PMID 9069287. doi:10.1038/386284a0
- Minakami R, Jinnai N, Sugiyama H (1997). «Phosphorylation and calmodulin binding of the metabotropic glutamate receptor subtype 5 (mGluR5) are antagonistic in vitro.». J. Biol. Chem. 272 (32): 20291–8. PMID 9242710. doi:10.1074/jbc.272.32.20291
- Snow BE, Hall RA, Krumins AM; et al. (1998). «GTPase activating specificity of RGS12 and binding specificity of an alternatively spliced PDZ (PSD-95/Dlg/ZO-1) domain.». J. Biol. Chem. 273 (28): 17749–55. PMID 9651375. doi:10.1074/jbc.273.28.17749
- Xiao B, Tu JC, Petralia RS; et al. (1998). «Homer regulates the association of group 1 metabotropic glutamate receptors with multivalent complexes of homer-related, synaptic proteins.». Neuron. 21 (4): 707–16. PMID 9808458. doi:10.1016/S0896-6273(00)80588-7
- Enz R (2002). «The actin-binding protein Filamin-A interacts with the metabotropic glutamate receptor type 7.». FEBS Lett. 514 (2-3): 184–8. PMID 11943148. doi:10.1016/S0014-5793(02)02361-X
- Saugstad JA, Yang S, Pohl J; et al. (2002). «Interaction between metabotropic glutamate receptor 7 and alpha tubulin.». J. Neurochem. 80 (6): 980–8. PMID 11953448. doi:10.1046/j.0022-3042.2002.00778.x
- Nash MS, Schell MJ, Atkinson PJ; et al. (2002). «Determinants of metabotropic glutamate receptor-5-mediated Ca2+ and inositol 1,4,5-trisphosphate oscillation frequency. Receptor density versus agonist concentration.». J. Biol. Chem. 277 (39): 35947–60. PMID 12119301. doi:10.1074/jbc.M205622200
- Bates B, Xie Y, Taylor N; et al. (2003). «Characterization of mGluR5R, a novel, metabotropic glutamate receptor 5-related gene.». Brain Res. Mol. Brain Res. 109 (1-2): 18–33. PMID 12531512. doi:10.1016/S0169-328X(02)00458-8
- Malherbe P, Kew JN, Richards JG; et al. (2003). «Identification and characterization of a novel splice variant of the metabotropic glutamate receptor 5 gene in human hippocampus and cerebellum.». Brain Res. Mol. Brain Res. 109 (1-2): 168–78. PMID 12531526. doi:10.1016/S0169-328X(02)00557-0
- O'Malley KL, Jong YJ, Gonchar Y; et al. (2003). «Activation of metabotropic glutamate receptor mGlu5 on nuclear membranes mediates intranuclear Ca2+ changes in heterologous cell types and neurons.». J. Biol. Chem. 278 (30): 28210–9. PMID 12736269. doi:10.1074/jbc.M300792200
- Corti C, Clarkson RW, Crepaldi L; et al. (2003). «Gene structure of the human metabotropic glutamate receptor 5 and functional analysis of its multiple promoters in neuroblastoma and astroglioma cells.». J. Biol. Chem. 278 (35): 33105–19. PMID 12783878. doi:10.1074/jbc.M212380200
- Aronica E, Gorter JA, Ijlst-Keizers H; et al. (2003). «Expression and functional role of mGluR3 and mGluR5 in human astrocytes and glioma cells: opposite regulation of glutamate transporter proteins.». Eur. J. Neurosci. 17 (10): 2106–18. PMID 12786977. doi:10.1046/j.1460-9568.2003.02657.x
- Uchino M, Sakai N, Kashiwagi K; et al. (2004). «Isoform-specific phosphorylation of metabotropic glutamate receptor 5 by protein kinase C (PKC) blocks Ca2+ oscillation and oscillatory translocation of Ca2+-dependent PKC.». J. Biol. Chem. 279 (3): 2254–61. PMID 14561742. doi:10.1074/jbc.M309894200
- Anneser JM, Ince PG, Shaw PJ, Borasio GD (2004). «Differential expression of mGluR5 in human lumbosacral motoneurons.». Neuroreport. 15 (2): 271–3. PMID 15076751. doi:10.1097/00001756-200402090-00012
- Pacheco R, Ciruela F, Casadó V; et al. (2004). «Group I metabotropic glutamate receptors mediate a dual role of glutamate in T cell activation.». J. Biol. Chem. 279 (32): 33352–8. PMID 15184389. doi:10.1074/jbc.M401761200
- Kim CH, Braud S, Isaac JT, Roche KW (2005). «Protein kinase C phosphorylation of the metabotropic glutamate receptor mGluR5 on Serine 839 regulates Ca2+ oscillations.». J. Biol. Chem. 280 (27): 25409–15. PMID 15894802. doi:10.1074/jbc.M502644200
- Cabello N, Remelli R, Canela L; et al. (2007). «Actin-binding protein alpha-actinin-1 interacts with the metabotropic glutamate receptor type 5b and modulates the cell surface expression and function of the receptor.». J. Biol. Chem. 282 (16): 12143–53. PMID 17311919. doi:10.1074/jbc.M608880200
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Classe A: Tipo rodopsina | Neurotransmissor | Adrenérgico | |
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Purinérgico | Adenosina ( A1, A2A, A2B, A3) · P2Y ( 1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14) |
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Serotonina | (todos, exceto 5-HT3) 5-HT1 ( A, B, D, E, F) · 5-HT2 ( A, B, C) · 5-HT ( 4, 5A, 6, 7) |
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Outros | Acetilcolina ( M1, M2, M3, M4, M5) · Dopamina ( D1, D2, D3, D4, D5) · Histamina ( H1, H2, H3, H4) · Melatonina ( 1A, 1B, 1C) · TAAR ( 1, 2, 3, 5, 6, 8, 9) |
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Metabólitos e moléculas de sinalização | Eicosanoide | CysLT ( 1, 2) · LTB4 ( 1, 2) · FPRL ( 1, 2, 3) · OXE · Prostaglandina ( DP ( 1, 2), EP ( 1, 2, 3, 4), FP) · Prostaciclina · Tromboxano |
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Outros | Ácido biliar · Ácido graxo livre ( 1, 2, 3, 4) · Ácido hidroxicarboxilíco ( 1, 2, 3) · Ácido lisofosfatídico ( 1, 2, 3, 4, 5, 6) · Canabinoide ( CB1, CB2, GPR ( 18, 55, 119)) · EBI2 · Estrogênio · Lisofosfolipídeo ( 1, 2, 3) · Oxoglutarato · PAF · Esfingosina-1-fosfato ( 1, 2, 3, 4, 5) · Succinato |
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Peptídeos | Neuropeptídeo | |
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Outros | Anafilatoxina ( C3a, C5a) · Angiotensina ( 1, 2) · Apelina · Bombesina ( BRS3, GRPR, NMBR) · Bradicinina ( B1, B2) · Quimiocina · Colecistoquinina ( A, B) · Endotelina ( A, B) · Formil peptídeo ( 1, 2, 3) · FSH · Galanina ( 1, 2, 3) · Receptor GHB · Hormônio liberador de gonadotrofina ( 1, 2) · Ghrelina · Kisspeptina · Hormônio luteinizante/coriogonadotropina · MAS ( 1, 1L, D, E, F, G, X1, X2, X3, X4) · Melanocortina ( 1, 2, 3, 4, 5) · MCHR ( 1, 2) · Motilina · Opioide ( δ, κ, μ, Nociceptina & ζ, mas não σ) · Orexina ( 1, 2) · Oxitocina · Procineticina ( 1, 2) · Peptídeo liberador de prolactina · Relaxina ( 1, 2, 3, 4) · Somatostatina ( 1, 2, 3, 4, 5) · Taquicinina ( 1, 2, 3) · Tirotrofina · Hormônio liberador de tirotropina · Urotensina-II · Vasopressina ( 1A, 1B, 2) |
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Miscelânea | Órfão | GPR ( 1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 81, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182, 183) |
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Outros | Olfatório · Opsina ( 3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) · Ativado por protease ( 1, 2, 3, 4) · SREB ( 1, 2, 3) |
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Classe B: Tipo secretina | Órfãos | GPR ( 56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157) |
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Outros | ADCYAP1R1 · Caderina ( 1, 2, 3) · Calcitonina · CALCRL · CD97 · EMR ( 1, 2, 3) · Glucagon ( GR, GIPR, GLP1R, GLP2R) · Hormônio liberador de corticotrofina ( 1, 2) · Hormônio liberador do hormônio do crescimento · Hormônio paratireoide ( 1, 2) · GPR · Inibidor de angiogênese específico do cérebro ( 1, 2, 3) · Latrofilina ( 1, 2, 3, ELTD1 · Peptídeo intestinal vasoativo ( 1, 2) · Proteínas tipo-Matusalém · Secretina |
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Classe C: Metabotrópico glutamato / feromona | Sabor | TAS1R ( 1, 2, 3) · TAS2R ( 1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 19, 20, 30, 31, 38, 39, 40, 41, 42, 43, 45, 46, 50) |
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Outros | Sensor de cálcio · GABA B ( 1, 2) · Glutamato ( Metabotrópico de glutamato ( 1, 2, 3, 4, 5, 6, 7, 8)) · GPRC6A · GPR ( 156, 158, 179) · RAIG ( 1, 2, 3, 4) |
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Class F: Frizzled / Smoothened | |
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