Biology:Tachykinin receptor 3

Short description: Protein-coding gene in the species Homo sapiens

Generic protein structure example

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

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.

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, K_i = 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, K_i = 13 nM, (R)-[(2-Phenyl-4-quinolinylcarbonyl)amino]-methyl ester benzeneacetic acid, CAS# 174635-53-1

See also

• Tachykinin receptor

Further reading

• "Tachykinins: receptor to effector". The International Journal of Biochemistry & Cell Biology 28 (7): 721–38. Jul 1996. doi:10.1016/1357-2725(96)00017-9. PMID 8925404. 
• "The role of tachykinin receptor antagonists in the prevention of bronchial hyperresponsiveness, airway inflammation and cough". The European Respiratory Journal 10 (8): 1892–906. Aug 1997. doi:10.1183/09031936.97.10081892. PMID 9272936. 
• "Molecular characterisation, expression and localisation of human neurokinin-3 receptor". FEBS Letters 299 (1): 90–5. Mar 1992. doi:10.1016/0014-5793(92)80107-R. PMID 1312036. 
• "The primary structure and gene organization of human substance P and neuromedin K receptors". European Journal of Biochemistry 204 (3): 1025–33. Mar 1992. doi:10.1111/j.1432-1033.1992.tb16724.x. PMID 1312928. 
• "Expression cloning of cDNA encoding a seven-helix receptor from human placenta with affinity for opioid ligands". Proceedings of the National Academy of Sciences of the United States of America 89 (9): 4124–8. May 1992. doi:10.1073/pnas.89.9.4124. PMID 1315051. Bibcode: 1992PNAS...89.4124X. 
• "cDNA sequence and heterologous expression of the human neurokinin-3 receptor". Biochemical and Biophysical Research Communications 184 (2): 966–72. Apr 1992. doi:10.1016/0006-291X(92)90685-E. PMID 1374246. 
• "Substance P and neurokinins as stimulants of the human isolated urinary bladder". Neuropeptides 11 (2): 83–7. 1988. doi:10.1016/0143-4179(88)90015-7. PMID 2452993. 
• "Functional expression of a novel human neurokinin-3 receptor homolog that binds [3Hsenktide and [125I-MePhe7]neurokinin B, and is responsive to tachykinin peptide agonists"]. Proceedings of the National Academy of Sciences of the United States of America 94 (1): 310–5. Jan 1997. doi:10.1073/pnas.94.1.310. PMID 8990205. Bibcode: 1997PNAS...94..310K. 
• "Tachykinin receptors on human monocytes: their involvement in rheumatoid arthritis". Neuropeptides 32 (3): 215–23. Jun 1998. doi:10.1016/S0143-4179(98)90040-3. PMID 10189055. 
• "Excessive placental secretion of neurokinin B during the third trimester causes pre-eclampsia". Nature 405 (6788): 797–800. Jun 2000. doi:10.1038/35015579. PMID 10866201. Bibcode: 2000Natur.405..797P. 
• "Pharmacological profile of the novel mammalian tachykinin, hemokinin 1". British Journal of Pharmacology 135 (1): 266–74. Jan 2002. doi:10.1038/sj.bjp.0704443. PMID 11786503. 
• "Tachykinins regulate the function of platelets". Blood 104 (4): 1058–65. Aug 2004. doi:10.1182/blood-2003-11-3979. PMID 15130944. 
• "Gene regulation of neurokinin B and its receptor NK3 in late pregnancy and pre-eclampsia". Molecular Human Reproduction 12 (7): 427–33. Jul 2006. doi:10.1093/molehr/gal025. PMID 16709596. 

External links

• "Tachykinin Receptors: NK₃". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=3031. 

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