Tachykinin receptor 3

{{Short description|Protein-coding gene in the species Homo sapiens}}

{{Infobox_gene}}

Tachykinin receptor 3, also known as TACR3, is a protein which in humans is encoded by the TACR3 gene.{{cite journal | vauthors = Huang RR, Cheung AH, Mazina KE, Strader CD, Fong TM | title = cDNA sequence and heterologous expression of the human neurokinin-3 receptor | journal = Biochemical and Biophysical Research Communications | volume = 184 | issue = 2 | pages = 966–72 | date = Apr 1992 | pmid = 1374246 | doi = 10.1016/0006-291X(92)90685-E }}{{cite web | title = Entrez Gene: TACR3 tachykinin receptor 3| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=6870}}

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.

Selective ligands

A number of selective ligands are available for NK3. NK3 receptor antagonists are being investigated as treatments for various indications.{{cite journal | vauthors = Quartara L, Altamura M | title = Tachykinin receptors antagonists: from research to clinic | journal = Current Drug Targets | volume = 7 | issue = 8 | pages = 975–92 | date = Aug 2006 | pmid = 16918326 | doi = 10.2174/138945006778019381 }}

= 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

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Further reading

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  • {{cite journal | vauthors = Khawaja AM, Rogers DF | title = Tachykinins: receptor to effector | journal = The International Journal of Biochemistry & Cell Biology | volume = 28 | issue = 7 | pages = 721–38 | date = Jul 1996 | pmid = 8925404 | doi = 10.1016/1357-2725(96)00017-9 }}
  • {{cite journal | vauthors = Advenier C, Lagente V, Boichot E | title = The role of tachykinin receptor antagonists in the prevention of bronchial hyperresponsiveness, airway inflammation and cough | journal = The European Respiratory Journal | volume = 10 | issue = 8 | pages = 1892–906 | date = Aug 1997 | pmid = 9272936 | doi = 10.1183/09031936.97.10081892 | doi-access = free }}
  • {{cite journal | vauthors = Buell G, Schulz MF, Arkinstall SJ, Maury K, Missotten M, Adami N, Talabot F, Kawashima E | title = Molecular characterisation, expression and localisation of human neurokinin-3 receptor | journal = FEBS Letters | volume = 299 | issue = 1 | pages = 90–5 | date = Mar 1992 | pmid = 1312036 | doi = 10.1016/0014-5793(92)80107-R | s2cid = 29031625 | doi-access = free }}
  • {{cite journal | vauthors = Takahashi K, Tanaka A, Hara M, Nakanishi S | title = The primary structure and gene organization of human substance P and neuromedin K receptors | journal = European Journal of Biochemistry | volume = 204 | issue = 3 | pages = 1025–33 | date = Mar 1992 | pmid = 1312928 | doi = 10.1111/j.1432-1033.1992.tb16724.x }}
  • {{cite journal | vauthors = Xie GX, Miyajima A, Goldstein A | title = Expression cloning of cDNA encoding a seven-helix receptor from human placenta with affinity for opioid ligands | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 89 | issue = 9 | pages = 4124–8 | date = May 1992 | pmid = 1315051 | pmc = 525645 | doi = 10.1073/pnas.89.9.4124 | bibcode = 1992PNAS...89.4124X | doi-access = free }}
  • {{cite journal | vauthors = Huang RR, Cheung AH, Mazina KE, Strader CD, Fong TM | title = cDNA sequence and heterologous expression of the human neurokinin-3 receptor | journal = Biochemical and Biophysical Research Communications | volume = 184 | issue = 2 | pages = 966–72 | date = Apr 1992 | pmid = 1374246 | doi = 10.1016/0006-291X(92)90685-E }}
  • {{cite journal | vauthors = Dion S, Corcos J, Carmel M, Drapeau G, Regoli D | title = Substance P and neurokinins as stimulants of the human isolated urinary bladder | journal = Neuropeptides | volume = 11 | issue = 2 | pages = 83–7 | year = 1988 | pmid = 2452993 | doi = 10.1016/0143-4179(88)90015-7 | s2cid = 13728584 }}
  • {{cite journal | vauthors = Krause JE, Staveteig PT, Mentzer JN, Schmidt SK, Tucker JB, Brodbeck RM, Bu JY, Karpitskiy VV | title = Functional expression of a novel human neurokinin-3 receptor homolog that binds [3H]senktide and [125I-MePhe7]neurokinin B, and is responsive to tachykinin peptide agonists | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 94 | issue = 1 | pages = 310–5 | date = Jan 1997 | pmid = 8990205 | pmc = 19326 | doi = 10.1073/pnas.94.1.310 | bibcode = 1997PNAS...94..310K | doi-access = free }}
  • {{cite journal | vauthors = Brunelleschi S, Bordin G, Colangelo D, Viano I | title = Tachykinin receptors on human monocytes: their involvement in rheumatoid arthritis | journal = Neuropeptides | volume = 32 | issue = 3 | pages = 215–23 | date = Jun 1998 | pmid = 10189055 | doi = 10.1016/S0143-4179(98)90040-3 | s2cid = 40222022 }}
  • {{cite journal | vauthors = Page NM, Woods RJ, Gardiner SM, Lomthaisong K, Gladwell RT, Butlin DJ, Manyonda IT, Lowry PJ | title = Excessive placental secretion of neurokinin B during the third trimester causes pre-eclampsia | journal = Nature | volume = 405 | issue = 6788 | pages = 797–800 | date = Jun 2000 | pmid = 10866201 | doi = 10.1038/35015579 | bibcode = 2000Natur.405..797P | s2cid = 4392048 }}
  • {{cite journal | vauthors = Bellucci F, Carini F, Catalani C, Cucchi P, Lecci A, Meini S, Patacchini R, Quartara L, Ricci R, Tramontana M, Giuliani S, Maggi CA | title = Pharmacological profile of the novel mammalian tachykinin, hemokinin 1 | journal = British Journal of Pharmacology | volume = 135 | issue = 1 | pages = 266–74 | date = Jan 2002 | pmid = 11786503 | pmc = 1573107 | doi = 10.1038/sj.bjp.0704443 }}
  • {{cite journal | vauthors = Graham GJ, Stevens JM, Page NM, Grant AD, Brain SD, Lowry PJ, Gibbins JM | title = Tachykinins regulate the function of platelets | journal = Blood | volume = 104 | issue = 4 | pages = 1058–65 | date = Aug 2004 | pmid = 15130944 | doi = 10.1182/blood-2003-11-3979 | doi-access = free }}
  • {{cite journal | vauthors = Page NM, Dakour J, Morrish DW | title = Gene regulation of neurokinin B and its receptor NK3 in late pregnancy and pre-eclampsia | journal = Molecular Human Reproduction | volume = 12 | issue = 7 | pages = 427–33 | date = Jul 2006 | pmid = 16709596 | doi = 10.1093/molehr/gal025 | doi-access = }}

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