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Tachykinin receptor 3: Wikis

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Tachykinin receptor 3
Identifiers
Symbols TACR3; MGC148060; MGC148061; NK3R; TAC3RL
External IDs OMIM162332 MGI892968 HomoloGene824 IUPHAR: NK3 GeneCards: TACR3 Gene
RNA expression pattern
PBB GE TACR3 208183 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 6870 21338
Ensembl ENSG00000169836 ENSMUSG00000028172
UniProt P29371 Q6NXX1
RefSeq (mRNA) NM_001059 NM_021382
RefSeq (protein) NP_001050 NP_067357
Location (UCSC) Chr 4:
104.73 - 104.86 Mb
Chr 3:
134.77 - 134.87 Mb
PubMed search [1] [2]

Tachykinin receptor 3, also known as TACR3, is a protein which in humans is encoded by the TACR3 gene.[1][2]

Contents

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.[2]

Selective ligands

Several selective ligands are available for NK3, with two compounds osanetant and talnetant currently in clinical trials for treatment of schizophrenia and other indications.[3]

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Agonists

  • Senktide - 7-amino acid polypeptide, NK3 selective, CAS# 106128-89-6

Antagonists

  • Osanetant
  • Talnetant
  • 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. ^ Huang RR, Cheung AH, Mazina KE, Strader CD, Fong TM (April 1992). "cDNA sequence and heterologous expression of the human neurokinin-3 receptor". Biochem. Biophys. Res. Commun. 184 (2): 966–72. doi:10.1016/0006-291X(92)90685-E. PMID 1374246.  
  2. ^ a b "Entrez Gene: TACR3 tachykinin receptor 3". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=6870.  
  3. ^ Quartara L, Altamura M (August 2006). "Tachykinin receptors antagonists: from research to clinic". Curr Drug Targets 7 (8): 975–92. doi:10.2174/138945006778019381. PMID 16918326.  

Further reading

  • Khawaja AM, Rogers DF (1996). "Tachykinins: receptor to effector.". Int. J. Biochem. Cell Biol. 28 (7): 721–38. doi:10.1016/1357-2725(96)00017-9. PMID 8925404.  
  • Advenier C, Lagente V, Boichot E (1997). "The role of tachykinin receptor antagonists in the prevention of bronchial hyperresponsiveness, airway inflammation and cough.". Eur. Respir. J. 10 (8): 1892–906. doi:10.1183/09031936.97.10081892. PMID 9272936.  
  • Buell G, Schulz MF, Arkinstall SJ, et al. (1992). "Molecular characterisation, expression and localisation of human neurokinin-3 receptor.". FEBS Lett. 299 (1): 90–5. doi:10.1016/0014-5793(92)80107-R. PMID 1312036.  
  • Takahashi K, Tanaka A, Hara M, Nakanishi S (1992). "The primary structure and gene organization of human substance P and neuromedin K receptors.". Eur. J. Biochem. 204 (3): 1025–33. doi:10.1111/j.1432-1033.1992.tb16724.x. PMID 1312928.  
  • Xie GX, Miyajima A, Goldstein A (1992). "Expression cloning of cDNA encoding a seven-helix receptor from human placenta with affinity for opioid ligands.". Proc. Natl. Acad. Sci. U.S.A. 89 (9): 4124–8. doi:10.1073/pnas.89.9.4124. PMID 1315051.  
  • Huang RR, Cheung AH, Mazina KE, et al. (1992). "cDNA sequence and heterologous expression of the human neurokinin-3 receptor.". Biochem. Biophys. Res. Commun. 184 (2): 966–72. doi:10.1016/0006-291X(92)90685-E. PMID 1374246.  
  • Dion S, Corcos J, Carmel M, et al. (1988). "Substance P and neurokinins as stimulants of the human isolated urinary bladder.". Neuropeptides 11 (2): 83–7. doi:10.1016/0143-4179(88)90015-7. PMID 2452993.  
  • Krause JE, Staveteig PT, Mentzer JN, et al. (1997). "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.". Proc. Natl. Acad. Sci. U.S.A. 94 (1): 310–5. doi:10.1073/pnas.94.1.310. PMID 8990205.  
  • Brunelleschi S, Bordin G, Colangelo D, Viano I (1999). "Tachykinin receptors on human monocytes: their involvement in rheumatoid arthritis.". Neuropeptides 32 (3): 215–23. doi:10.1016/S0143-4179(98)90040-3. PMID 10189055.  
  • Page NM, Woods RJ, Gardiner SM, et al. (2000). "Excessive placental secretion of neurokinin B during the third trimester causes pre-eclampsia.". Nature 405 (6788): 797–800. doi:10.1038/35015579. PMID 10866201.  
  • Bellucci F, Carini F, Catalani C, et al. (2002). "Pharmacological profile of the novel mammalian tachykinin, hemokinin 1.". Br. J. Pharmacol. 135 (1): 266–74. doi:10.1038/sj.bjp.0704443. PMID 11786503.  
  • Strausberg RL, Feingold EA, Grouse LH, et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMID 12477932.  
  • Graham GJ, Stevens JM, Page NM, et al. (2005). "Tachykinins regulate the function of platelets.". Blood 104 (4): 1058–65. doi:10.1182/blood-2003-11-3979. PMID 15130944.  
  • Gerhard DS, Wagner L, Feingold EA, et al. (2004). "The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).". Genome Res. 14 (10B): 2121–7. doi:10.1101/gr.2596504. PMID 15489334.  
  • Page NM, Dakour J, Morrish DW (2006). "Gene regulation of neurokinin B and its receptor NK3 in late pregnancy and pre-eclampsia.". Mol. Hum. Reprod. 12 (7): 427–33. doi:10.1093/molehr/gal025. PMID 16709596.  

External links

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


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