Oreksinski receptor 2

Hipokretinski (oreksinski) receptor 2
Identifikatori
Simboli	HCRTR2; OX2R
Vanjski ID	OMIM: 602393 MGI: 2680765 HomoloGene: 1168 IUPHAR: OX2 GeneCards: HCRTR2 Gene
Ontologija gena
Molekularna funkcija	• aktivnost rodopsinu-sličnog receptora; • receptorska aktivnost; • aktivnost neuropeptidnog receptora; • aktivnost oreksinskog receptora;
Celularna komponenta	• integralno sa ćelijskom membranom; • membrana;
Biološki proces	• prenos signala; • G-proteinska signalizacija, spregnuto sa IP3 sekundarnim glasnikom (aktivacija fosfolipaze C); • neuropeptidni signalni put; • sinapsna transmisija; • ishrana;
Pregled RNK izražavanja
	podaci
Ortolozi

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

Funkcija

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

Agonisti

Oreksin-A
Oreksin-B
SB-668,875

Antagonisti

Almoreksant - nespecifični OX_1/2 antagonist
SB-649,868 - nespecifični OX_1/2 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]

Povezano

Oreksinski receptor

Reference

↑ ^1,0 ^1,1 „Entrez Gene: HCRTR2 hypocretin (orexin) receptor 2”.
↑ McAtee, LC; Sutton, SW; Rudolph, DA; Li, X; Aluisio, LE; Phuong, VK; Dvorak, CA; Lovenberg, TW i dr.. (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.
↑ Cole, AG; Stroke, IL; Qin, LY; Hussain, Z; Simhadri, S; Brescia, MR; Waksmunski, FS; Strohl, B i dr.. (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.

Literatura

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 18213. 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. Arhivirano iz originala na datum 2011-07-11. Pristupljeno 2014-05-08.
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 310948. 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 139241. PMID 12477932.

Spoljašnje veze

„Orexin Receptors: OX₂”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano iz originala na datum 2012-10-23.

[entrez-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 i dr.. (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 i dr.. (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.

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