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Tachykinin receptor 2

From Wikipedia, the free encyclopedia
TACR2
Identifiers
AliasesTACR2, NK2R, NKNAR, SKR, TAC2R, Tachykinin receptor 2
External IDsOMIM: 162321; MGI: 98477; HomoloGene: 55548; GeneCards: TACR2; OMA:TACR2 - orthologs
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_001057

NM_009314

RefSeq (protein)

NP_001048

NP_033340

Location (UCSC)Chr 10: 69.4 – 69.42 MbChr 10: 62.09 – 62.1 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse

Substance-K receptor is a protein that in humans is encoded by the TACR2 gene.[5]

Function

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This gene belongs to a family of genes that function as receptors for tachykinins. Receptor affinities are specified by variations in the 5'-end of the sequence. The receptors belonging to this family are characterized by interactions with G proteins and 7 hydrophobic transmembrane regions. This gene encodes the receptor for the tachykinin neuropeptide substance K, also referred to as neurokinin A.[5]

Selective Ligands

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Several selective ligands for NK2 are now available, and although most of the compounds developed so far are peptides, one small-molecule antagonist Saredutant is currently in clinical trials as an anxiolytic and antidepressant.

Agonists

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  • GR-64349 - potent and selective agonist, EC50 3.7nM, 7-amino acid polypeptide chain. CAS# 137593-52-3

Antagonists

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  • Ibodutant - failed its Phase 3 trial for IBS treatment in 2015, and abandoned by Menarini
  • Saredutant - mixed but mostly negative Phase 3 trial results in 2009, and abandoned by Sanofi-Aventis
  • GR-159897
  • MEN-10376 - potent and selective antagonist, 7-amino acid polypeptide chain. CAS# 135306-85-3

See also

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References

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  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000075073Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000020081Ensembl, May 2017
  3. ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ^ a b "Entrez Gene: TACR2 tachykinin receptor 2".

Further reading

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[edit]
  • "Tachykinin Receptors: NK2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from the original on 2012-05-31. Retrieved 2008-12-09.

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