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词条 Neuromedin U receptor
释义

  1. Selective Ligands

     Agonists  Antagonists 

  2. References

  3. External links

{{infobox protein
| Name = neuromedin U receptor 1
| caption =
| image =
| width =
| HGNCid = 4518
| Symbol = NMUR1
| AltSymbols = GPR66
| EntrezGene = 10316
| OMIM = 604153
| RefSeq = NM_006056
| UniProt = Q9HB89
| PDB =
| ECnumber =
| Chromosome = 2
| Arm = q
| Band = 37.1
| LocusSupplementaryData =
}}{{infobox protein
| Name = neuromedin U receptor 2
| caption =
| image =
| width =
| HGNCid = 16454
| Symbol = NMUR2
| AltSymbols = NMU2R
| EntrezGene = 56923
| OMIM = 605108
| RefSeq = NM_020167
| UniProt = Q9GZQ4
| PDB =
| ECnumber =
| Chromosome = 5
| Arm = q
| Band = 33.1
| LocusSupplementaryData =
}}

The neuromedin U receptors are two G-protein coupled receptors which bind the neuropeptide hormones neuromedin U and neuromedin S.[1] There are two subtypes of the neuromedin U receptor, each encoded by a separate gene ({{gene|NMUR1}}, {{gene|NMUR2}}).

Selective Ligands

Neuromedin U is an agonist at both the NMU1 and NMU2 subtypes, while neuromedin S is selective for NMU2, and is a more potent agonist at this subtype than neuromedin U.[2][3] Several other peptide and non-peptide ligands are also available for the NMU receptors.

Agonists

Non-selective
  • Neuromedin U
  • non-peptide NMU modulators [4][5]
NMU2 selective
  • Neuromedin S

Antagonists

NMU2 selective
  • R-PSOP [6]

References

1. ^{{cite journal |vauthors=Brighton PJ, Szekeres PG, Willars GB |title=Neuromedin U and its receptors: structure, function, and physiological roles |journal=Pharmacological Reviews |volume=56 |issue=2 |pages=231–48 |date=June 2004 |pmid=15169928 |doi=10.1124/pr.56.2.3 |url=}}
2. ^{{cite journal |vauthors=Mitchell J, Maguire J, Davenport A |title=Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin S |journal=British Journal of Pharmacology |volume= 158|issue= 1|pages= 87–103|date=June 2009 |pmid=19519756 |doi=10.1111/j.1476-5381.2009.00252.x |url= |pmc=2795236}}
3. ^{{cite journal |vauthors=Peier A, Kosinski J, Cox-York K, Qian Y, Desai K, Feng Y, Trivedi P, Hastings N, Marsh DJ |title=The antiobesity effects of centrally administered neuromedin U and neuromedin S are mediated predominantly by the neuromedin U receptor 2 (NMUR2) |journal=Endocrinology |volume=150 |issue=7 |pages=3101–9 |date=July 2009 |pmid=19324999 |doi=10.1210/en.2008-1772 |url= |pmc=2703546}}
4. ^{{cite journal |vauthors=Meng T, Su HR, Binkert C, Fischli W, Zhou L, Shen JK, Wang MW |title=Identification of non-peptidic neuromedin U receptor modulators by a robust homogeneous screening assay |journal=Acta Pharmacologica Sinica |volume=29 |issue=4 |pages=517–27 |date=April 2008 |pmid=18358099 |doi= 10.1111/j.1745-7254.2008.00769.x|url=}}
5. ^Kajino M, Hinuma S, Tarui N, Yamashita T, Nakayama Y. Receptor regulators. European Patent EP 1559428 A1. Published 03.08.2005
6. ^{{cite journal |vauthors=Liu JJ, Payza K, Huang J, Liu R, Chen T, Coupal M, Laird JM, Cao CQ, Butterworth J, Lapointe S, Bayrakdarian M, Trivedi S, Bostwick JR |title=Discovery and pharmacological characterization of a small-molecule antagonist at neuromedin U receptor NMUR2 |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=330 |issue=1 |pages=268–75 |date=July 2009 |pmid=19369576 |doi=10.1124/jpet.109.152967 |url=}}

External links

  • {{cite web | url = http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1312 | title = Neuromedin U Receptors | accessdate = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | language = | archiveurl = | archivedate = | quote = }}
  • {{MeshName|Neuromedin+U+Receptor}}
{{G protein-coupled receptors}}{{transmembranereceptor-stub}}

1 : G protein-coupled receptors

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