Tachykinin receptor 3
Tachykinin receptor 3, also known as TACR3, is a protein which in humans is encoded by the TACR3 gene.[1][2]
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. Two compounds osanetant and talnetant are being developed for treatment of various indications.[3]
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
- ↑ 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.
- ↑ 2.0 2.1 "Entrez Gene: TACR3 tachykinin receptor 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. PMC 525645. 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 3Hsenktide and 125I-MePhe7neurokinin 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. PMC 19326. 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. PMC 1573107. 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. PMC 139241. 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. PMC 528928. 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
- "Tachykinin Receptors: NK3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
| ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||