Biology:Neuromedin U receptor

From HandWiki
Short description: InterPro Family
neuromedin U receptor 1
Identifiers
SymbolNMUR1
Alt. symbolsGPR66
NCBI gene10316
HGNC4518
OMIM604153
RefSeqNM_006056
UniProtQ9HB89
Other data
LocusChr. 2 q37.1
neuromedin U receptor 2
Identifiers
SymbolNMUR2
Alt. symbolsNMU2R
NCBI gene56923
HGNC16454
OMIM605108
RefSeqNM_020167
UniProtQ9GZQ4
Other data
LocusChr. 5 q33.1

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 (NMUR1, 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
NMU2 selective

Antagonists

NMU2 selective

References

  1. "Neuromedin U and its receptors: structure, function, and physiological roles". Pharmacological Reviews 56 (2): 231–48. June 2004. doi:10.1124/pr.56.2.3. PMID 15169928. 
  2. "Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin S". British Journal of Pharmacology 158 (1): 87–103. June 2009. doi:10.1111/j.1476-5381.2009.00252.x. PMID 19519756. 
  3. "The antiobesity effects of centrally administered neuromedin U and neuromedin S are mediated predominantly by the neuromedin U receptor 2 (NMUR2)". Endocrinology 150 (7): 3101–9. July 2009. doi:10.1210/en.2008-1772. PMID 19324999. 
  4. "Identification of non-peptidic neuromedin U receptor modulators by a robust homogeneous screening assay". Acta Pharmacologica Sinica 29 (4): 517–27. April 2008. doi:10.1111/j.1745-7254.2008.00769.x. PMID 18358099. 
  5. Kajino M, Hinuma S, Tarui N, Yamashita T, Nakayama Y. Receptor regulators. European Patent EP 1559428 A1. Published 03.08.2005
  6. "Discovery and pharmacological characterization of a small-molecule antagonist at neuromedin U receptor NMUR2". The Journal of Pharmacology and Experimental Therapeutics 330 (1): 268–75. July 2009. doi:10.1124/jpet.109.152967. PMID 19369576. 

External links