Tachykinin receptor 3

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TACR3
Identifiers
AliasesTACR3, HH11, NK-3R, NK3R, NKR, TAC3RL, Tachykinin receptor 3, TAC3R, NK3
External IDsMGI: 892968 HomoloGene: 824 GeneCards: TACR3
Gene location (Human)
Chromosome 4 (human)
Chr.Chromosome 4 (human)[1]
Chromosome 4 (human)
Genomic location for TACR3
Genomic location for TACR3
Band4q24Start103,586,031 bp[1]
End103,719,816 bp[1]
RNA expression pattern
PBB GE TACR3 208183 at fs.png
More reference expression data
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_001059

NM_021382

RefSeq (protein)

NP_001050

NP_067357

Location (UCSC)Chr 4: 103.59 – 103.72 MbChr 3: 134.83 – 134.93 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse

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

Function[edit]

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[edit]

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

Agonists[edit]

  • 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[edit]

  • 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[edit]

References[edit]

  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000169836 - Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000028172 - Ensembl, May 2017
  3. ^ "Human PubMed Reference:". 
  4. ^ "Mouse PubMed Reference:". 
  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. ^ a b "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[edit]

External links[edit]

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