Neuromedin U receptor

{{Short description|InterPro Family}}

{{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.{{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 |s2cid=884735 }} 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.{{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 |pmc=2795236}}{{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 |pmc=2703546}} Several other peptide and non-peptide ligands are also available for the NMU receptors.

=Agonists=

;Non-selective

  • Neuromedin U
  • non-peptide NMU modulators {{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|doi-access=free }}Kajino M, Hinuma S, Tarui N, Yamashita T, Nakayama Y. Receptor regulators. European Patent EP 1559428 A1. Published 03.08.2005

;NMU2 selective

=Antagonists=

;NMU2 selective

  • R-PSOP {{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 |s2cid=7366636 }}

References

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