Hypocretin (orexin) receptor 2

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Hypocretin (orexin) receptor 2
Available structures
PDB Ortholog search: PDBe, RCSB
Identifiers
Symbols HCRTR2 ; OX2R
External IDs OMIM602393 MGI2680765 HomoloGene1168 IUPHAR: 322 ChEMBL: 4792 GeneCards: HCRTR2 Gene
RNA expression pattern
PBB GE HCRTR2 207393 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 3062 387285
Ensembl ENSG00000137252 ENSMUSG00000032360
UniProt O43614 P58308
RefSeq (mRNA) NM_001526 NM_198962
RefSeq (protein) NP_001517 NP_945200
Location (UCSC) Chr 6:
55.11 – 55.28 Mb
Chr 9:
76.23 – 76.32 Mb
PubMed search [1] [2]
Orexin receptor type 2
Identifiers
Symbol Orexin_rec2
Pfam PF03827
InterPro IPR004060

Orexin receptor type 2 (Ox2R or OX2), also known as hypocretin receptor type 2, is a protein that in humans is encoded by the HCRTR2 gene.[1]

Function[edit]

OX2 is a G-protein coupled receptor expressed exclusively in the brain. It has 64% identity with OX1. OX2 binds both orexin A and orexin B neuropeptides. OX2 is involved in the central feedback mechanism that regulates feeding behaviour.[1]

Ligands[edit]

Agonists[edit]

Antagonists[edit]

See also[edit]

References[edit]

  1. ^ a b "Entrez Gene: HCRTR2 hypocretin (orexin) receptor 2". 
  2. ^ McAtee LC, Sutton SW, Rudolph DA, Li X, Aluisio LE, Phuong VK et al. (Aug 2004). "Novel substituted 4-phenyl-[1,3]dioxanes: 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. ^ Roecker AJ, Mercer SP, Schreier JD, Cox CD, Fraley ME, Steen JT et al. (Feb 2014). "Discovery of 5-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia". ChemMedChem 9 (2): 311–22. doi:10.1002/cmdc.201300447. PMID 24376006. 
  4. ^ Kuduk SD, Skudlarek JW, DiMarco CN, Bruno JG, Pausch MH, O'Brien JA et al. (Jun 2015). "Identification of MK-8133: An orexin-2 selective receptor antagonist with favorable development properties". Bioorganic & Medicinal Chemistry Letters 25 (12): 2488–92. doi:10.1016/j.bmcl.2015.04.066. PMID 25981685. 
  5. ^ Cole AG, Stroke IL, Qin LY, Hussain Z, Simhadri S, Brescia MR et al. (Oct 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. 
  6. ^ Fujimoto T, Kunitomo J, Tomata Y, Nishiyama K, Nakashima M, Hirozane M et al. (Nov 2011). "Discovery of potent, selective, orally active benzoxazepine-based Orexin-2 receptor antagonists". Bioorganic & Medicinal Chemistry Letters 21 (21): 6414–6. doi:10.1016/j.bmcl.2011.08.093. PMID 21917455. 

Further reading[edit]

This article incorporates text from the United States National Library of Medicine, which is in the public domain.