Oreksinski receptor 2

Из Википедије, слободне енциклопедије
Hipokretinski (oreksinski) receptor 2
Identifikatori
Simboli HCRTR2; OX2R
Vanjski ID OMIM602393 MGI2680765 HomoloGene1168 IUPHAR: OX2 GeneCards: HCRTR2 Gene
Pregled RNK izražavanja
PBB GE HCRTR2 207393 at tn.png
podaci
Ortolozi
Vrsta Čovek Miš
Entrez 3062 387285
Ensembl ENSG00000137252 ENSMUSG00000032360
UniProt O43614 Q8BV78
RefSeq (mRNA) NM_001526 NM_198962
RefSeq (protein) NP_001517 NP_945200
Lokacija (UCSC) Chr 6:
55.15 - 55.26 Mb
Chr 9:
76.01 - 76.11 Mb
PubMed pretraga [1] [2]

Oreksinski receptor tip 2 (OX2R, OX2, ili hipokretinski receptor tip 2), je protein koji je kod ljudi kodiran HCRTR2 genom.[1]

Funkcija[уреди]

OX2 je G-protein spregnuti receptor koji je isključivo izražen u mozgu. On je 64% identičan s OX1. OX2 vezuje oreksin A i oreksin B neuropeptide. OX2 učestvuje u centralnom povratnom mehanizmu koji reguliše unos hrane.[1]

Ligandi[уреди]

Agonisti[уреди]

Antagonisti[уреди]

  • Almoreksant - nespecifični OX1/2 antagonist
  • SB-649,868 - nespecifični OX1/2 antagonist
  • TCS-OX2-29 - selektivni OX2 antagonist
  • 1-(2,4-dibromofenil)-3-((4S,5S)-2,2-dimetil-4-fenil-[1,3]dioksan-5-il)urea (600 puta selektivniji za OX2 od OX1)[2]
  • (3,4-dimetoksifenoksi)alkilamino acetamidi[3]

Vidi još[уреди]

Literatura[уреди]

  1. 1,0 1,1 „Entrez Gene: HCRTR2 hypocretin (orexin) receptor 2”. 
  2. McAtee, LC; Sutton, SW; Rudolph, DA; Li, X; Aluisio, LE; Phuong, VK; Dvorak, CA; Lovenberg, TW; Carruthers, NI (2004). „Novel substituted 4-phenyl-1,3dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists”. Bioorganic & medicinal chemistry letters. 14 (16): 4225—9. doi:10.1016/j.bmcl.2004.06.032. PMID 15261275. 
  3. Cole, AG; Stroke, IL; Qin, LY; Hussain, Z; Simhadri, S; Brescia, MR; Waksmunski, FS; Strohl, B; Tellew, JE (2008). „Synthesis of (3,4-dimethoxyphenoxy)alkylamino acetamides as orexin-2 receptor antagonists”. Bioorganic & medicinal chemistry letters. 18 (20): 5420—3. doi:10.1016/j.bmcl.2008.09.038. PMID 18815029. 

Dodatna literatura[уреди]

  • Flier JS, Maratos-Flier E (1998). „Obesity and the hypothalamus: novel peptides for new pathways.”. Cell. 92 (4): 437—40. doi:10.1016/S0092-8674(00)80937-X. PMID 9491885. 
  • Willie JT, Chemelli RM, Sinton CM, Yanagisawa M (2001). „To eat or to sleep? Orexin in the regulation of feeding and wakefulness.”. Annu. Rev. Neurosci. 24: 429—58. doi:10.1146/annurev.neuro.24.1.429. PMID 11283317. 
  • Hungs M, Mignot E (2001). „Hypocretin/orexin, sleep and narcolepsy.”. Bioessays. 23 (5): 397—408. doi:10.1002/bies.1058. PMID 11340621. 
  • de Lecea L, Kilduff TS, Peyron C; et al. (1998). „The hypocretins: hypothalamus-specific peptides with neuroexcitatory activity.”. Proc. Natl. Acad. Sci. U.S.A. 95 (1): 322—7. doi:10.1073/pnas.95.1.322. PMC 18213слободно за читање. PMID 9419374. 
  • Sakurai T, Amemiya A, Ishii M; et al. (1998). „Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior.” (PDF). Cell. 92 (4): 573—85. doi:10.1016/S0092-8674(00)80949-6. PMID 9491897. 
  • Sakurai T, Amemiya A, Ishii M; et al. (1998). „Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior.”. Cell. 92 (5): 697. doi:10.1016/S0092-8674(02)09256-5. PMID 9527442. 
  • Peyron C, Faraco J, Rogers W; et al. (2000). „A mutation in a case of early onset narcolepsy and a generalized absence of hypocretin peptides in human narcoleptic brains.”. Nat. Med. 6 (9): 991—7. doi:10.1038/79690. PMID 10973318. 
  • Wright GJ, Puklavec MJ, Willis AC; et al. (2000). „Lymphoid/neuronal cell surface OX2 glycoprotein recognizes a novel receptor on macrophages implicated in the control of their function.”. Immunity. 13 (2): 233—42. doi:10.1016/S1074-7613(00)00023-6. PMID 10981966. 
  • Hartley JL, Temple GF, Brasch MA (2001). „DNA cloning using in vitro site-specific recombination.”. Genome Res. 10 (11): 1788—95. doi:10.1101/gr.143000. PMC 310948слободно за читање. PMID 11076863. 
  • Mazzocchi G, Malendowicz LK, Gottardo L; et al. (2001). „Orexin A stimulates cortisol secretion from human adrenocortical cells through activation of the adenylate cyclase-dependent signaling cascade.”. J. Clin. Endocrinol. Metab. 86 (2): 778—82. doi:10.1210/jc.86.2.778. PMID 11158046. 
  • Blanco M, López M, García-Caballero T; et al. (2001). „Cellular localization of orexin receptors in human pituitary.”. J. Clin. Endocrinol. Metab. 86 (4): 1616—9. doi:10.1210/jc.86.4.1616. PMID 11297593. 
  • Blanco M, López M, GarcIa-Caballero T; et al. (2001). „Cellular localization of orexin receptors in human pituitary.”. J. Clin. Endocrinol. Metab. 86 (7): 3444—7. doi:10.1210/jc.86.7.3444. PMID 11443222. 
  • Karteris E, Randeva HS, Grammatopoulos DK; et al. (2001). „Expression and coupling characteristics of the CRH and orexin type 2 receptors in human fetal adrenals.”. J. Clin. Endocrinol. Metab. 86 (9): 4512—9. doi:10.1210/jc.86.9.4512. PMID 11549701. 
  • Randeva HS, Karteris E, Grammatopoulos D, Hillhouse EW (2001). „Expression of orexin-A and functional orexin type 2 receptors in the human adult adrenals: implications for adrenal function and energy homeostasis.”. J. Clin. Endocrinol. Metab. 86 (10): 4808—13. doi:10.1210/jc.86.10.4808. PMID 11600545. 
  • Olafsdóttir BR, Rye DB, Scammell TE; et al. (2002). „Polymorphisms in hypocretin/orexin pathway genes and narcolepsy.”. Neurology. 57 (10): 1896—9. PMID 11723285. 
  • Blanco M, García-Caballero T, Fraga M; et al. (2002). „Cellular localization of orexin receptors in human adrenal gland, adrenocortical adenomas and pheochromocytomas.”. Regul. Pept. 104 (1-3): 161—5. doi:10.1016/S0167-0115(01)00359-7. PMID 11830291. 
  • Strausberg RL, Feingold EA, Grouse LH; et al. (2003). „Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.”. Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899—903. doi:10.1073/pnas.242603899. PMC 139241слободно за читање. PMID 12477932. 

Spoljašnje veze[уреди]

  • „Orexin Receptors: OX2. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.