Tachykinin receptor 3

Tachykinin receptor 3, also known as TACR3, is a protein which in humans is encoded by the TACR3 gene.[5][6]

TACR3
Identifiers
AliasesTACR3, HH11, NK-3R, NK3R, NKR, TAC3RL, Tachykinin receptor 3, TAC3R, NK3
External IDsOMIM: 162332 MGI: 892968 HomoloGene: 824 GeneCards: TACR3
Orthologs
SpeciesHumanMouse
Entrez

6870

21338

Ensembl

ENSG00000169836

ENSMUSG00000028172

UniProt

P29371

P47937

RefSeq (mRNA)

NM_001059

NM_021382

RefSeq (protein)

NP_001050

NP_067357

Location (UCSC)Chr 4: 103.59 – 103.72 MbChr 3: 134.53 – 134.64 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse

Function

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 neurokinin 3, also referred to as neurokinin B.[6]

Selective ligands

A number of selective ligands are available for NK3. NK3 receptor antagonists are being investigated as treatments for various indications.[7]

Agonists

  • Neurokinin B – endogenous peptide ligand, also interacts with other neurokinin receptors but has highest affinity for NK3
  • Senktide – 7-amino acid polypeptide, NK3 selective, CAS# 106128-89-6

Antagonists

  • Elinzanetant (BAY-3427080 GSK-1144814, NT-814)
  • Fezolinetant (ESN-364)
  • Osanetant (SR-142,801)
  • Pavinetant (MLE-4901, AZD-4901, AZD-2624)
  • Talnetant (SB-223,412)
  • SB-222,200 – potent and selective antagonist, Ki = 4.4 nM, 3-Methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide, CAS# 174635-69-9
  • SB-218,795 – more selective than SB-222,200, Ki = 13 nM, (R)-[(2-Phenyl-4-quinolinylcarbonyl)amino]-methyl ester benzeneacetic acid, CAS# 174635-53-1

See also

References

  1. GRCh38: Ensembl release 89: ENSG00000169836 - Ensembl, May 2017
  2. GRCm38: Ensembl release 89: ENSMUSG00000028172 - Ensembl, 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. Huang RR, Cheung AH, Mazina KE, Strader CD, Fong TM (Apr 1992). "cDNA sequence and heterologous expression of the human neurokinin-3 receptor". Biochemical and Biophysical Research Communications. 184 (2): 966–72. doi:10.1016/0006-291X(92)90685-E. PMID 1374246.
  6. "Entrez Gene: TACR3 tachykinin receptor 3".
  7. Quartara L, Altamura M (Aug 2006). "Tachykinin receptors antagonists: from research to clinic". Current Drug Targets. 7 (8): 975–92. doi:10.2174/138945006778019381. PMID 16918326.

Further reading

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


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