Oreksinski receptor 2

Hipokretinski (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
Vrsta	Čovek
Entrez	3062
Ensembl	ENSG00000137252
UniProt	O43614
RefSeq (mRNA)	NM_001526
RefSeq (protein)	NP_001517
Lokacija (UCSC)	Chr 6:; 55.15 - 55.26 Mb
PubMed pretraga	[1]

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]

Vidi još

Oreksinski receptor

Literatura

^ ^а ^б „Entrez Gene: HCRTR2 hypocretin (orexin) receptor 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. PMID 15261275. doi:10.1016/j.bmcl.2004.06.032.
^ 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. PMID 18815029. doi:10.1016/j.bmcl.2008.09.038.

Dodatna literatura

Flier JS, Maratos-Flier E (1998). „Obesity and the hypothalamus: novel peptides for new pathways.”. Cell. 92 (4): 437—40. PMID 9491885. doi:10.1016/S0092-8674(00)80937-X.
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. PMID 11283317. doi:10.1146/annurev.neuro.24.1.429.
Hungs M, Mignot E (2001). „Hypocretin/orexin, sleep and narcolepsy.”. Bioessays. 23 (5): 397—408. PMID 11340621. doi:10.1002/bies.1058.
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. PMC 18213 . PMID 9419374. doi:10.1073/pnas.95.1.322.
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. PMID 9491897. doi:10.1016/S0092-8674(00)80949-6. Архивирано из оригинала (PDF) 11. 07. 2011. г. Приступљено 22. 04. 2011.
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. PMID 9527442. doi:10.1016/S0092-8674(02)09256-5.
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. PMID 10973318. doi:10.1038/79690.
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. PMID 10981966. doi:10.1016/S1074-7613(00)00023-6.
Hartley JL, Temple GF, Brasch MA (2001). „DNA cloning using in vitro site-specific recombination.”. Genome Res. 10 (11): 1788—95. PMC 310948 . PMID 11076863. doi:10.1101/gr.143000.
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. PMID 11158046. doi:10.1210/jc.86.2.778.
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. PMID 11297593. doi:10.1210/jc.86.4.1616.
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. PMID 11443222. doi:10.1210/jc.86.7.3444.
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. PMID 11549701. doi:10.1210/jc.86.9.4512.
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. PMID 11600545. doi:10.1210/jc.86.10.4808.
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. PMID 11830291. doi:10.1016/S0167-0115(01)00359-7.
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. PMC 139241 . PMID 12477932. doi:10.1073/pnas.242603899.

Spoljašnje veze

„Orexin Receptors: OX₂”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Архивирано из оригинала 23. 10. 2012. г.

[entrez-1] а ^б „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. PMID 15261275. doi:10.1016/j.bmcl.2004.06.032.

[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. PMID 18815029. doi:10.1016/j.bmcl.2008.09.038.

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