Tachykinin receptor 3: Difference between revisions
m Robot: Automated text replacement (-{{reflist}} +{{reflist|2}}, -<references /> +{{reflist|2}}, -{{WikiDoc Cardiology Network Infobox}} +) |
m Bot: HTTP→HTTPS (v470) |
||
Line 1: | Line 1: | ||
{{Infobox_gene}} | |||
'''Tachykinin receptor 3''', also known as '''TACR3''', is a [[protein]] which in humans is encoded by the ''TACR3'' [[gene]].<ref name="pmid1374246">{{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 }}</ref><ref name="entrez">{{cite web | title = Entrez Gene: TACR3 tachykinin receptor 3| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=6870| accessdate = }}</ref> | |||
== Function == | |||
This gene belongs to a family of genes that function as [[receptor (biochemistry)|receptor]]s for [[tachykinin]]s. 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]].<ref name="entrez" /> | |||
== Selective ligands == | |||
A number of selective ligands are available for NK<sub>3</sub>. NK<sub>3</sub> receptor antagonists are being investigated as treatments for various indications.<ref name="pmid16918326">{{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 }}</ref> | |||
=== Agonists === | |||
* [[Neurokinin B]] – endogenous peptide ligand, also interacts with other neurokinin receptors but has highest affinity for NK<sub>3</sub> | |||
* [[Senktide]] – 7-amino acid polypeptide, NK<sub>3</sub> selective, CAS# 106128-89-6 | |||
==See also== | === Antagonists === | ||
* [[Fezolinetant]] (ESN-364) | |||
* [[MLE-4901]] (also known as AZD-4901, formerly AZD-2624) | |||
* [[Osanetant]] (SR-142,801) | |||
* [[Talnetant]] (SB-223,412) | |||
* [[SB-222,200]] – potent and selective antagonist, K<sub>i</sub> = 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<sub>i</sub> = 13 nM, (R)-[(2-Phenyl-4-quinolinylcarbonyl)amino]-methyl ester benzeneacetic acid, CAS# 174635-53-1 | |||
== See also == | |||
* [[Tachykinin receptor]] | * [[Tachykinin receptor]] | ||
==References== | == References == | ||
{{reflist| | {{reflist|35em}} | ||
==Further reading== | == Further reading == | ||
{{refbegin | | {{refbegin|35em}} | ||
* {{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 }} | |||
*{{cite journal | * {{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 }} | ||
*{{cite journal | * {{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 / FEBS | volume = 204 | issue = 3 | pages = 1025–33 | date = Mar 1992 | pmid = 1312928 | doi = 10.1111/j.1432-1033.1992.tb16724.x }} | ||
*{{cite journal | * {{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 }} | ||
*{{cite journal | * {{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 | * {{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 }} | ||
*{{cite journal | * {{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 }} | ||
*{{cite journal | * {{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 }} | ||
*{{cite journal | * {{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 }} | ||
*{{cite journal | * {{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 | * {{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 }} | ||
*{{cite journal | * {{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 }} | ||
*{{cite journal | |||
*{{cite journal | |||
}} | |||
{{refend}} | {{refend}} | ||
== External links == | |||
* {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=3031 | title = Tachykinin Receptors: NK<sub>3</sub> | accessdate = | author = | authorlink = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | archiveurl = | archivedate = | quote = }} | |||
{{NLM content}} | {{NLM content}} | ||
{{G protein-coupled receptors}} | {{G protein-coupled receptors}} | ||
{{Neurokinin receptor modulators}} | |||
[[Category:G protein coupled receptors]] | [[Category:G protein coupled receptors]] | ||
{{ | {{transmembranereceptor-stub}} |
Revision as of 00:57, 27 October 2017
VALUE_ERROR (nil) | |||||||
---|---|---|---|---|---|---|---|
Identifiers | |||||||
Aliases | |||||||
External IDs | GeneCards: [1] | ||||||
Orthologs | |||||||
Species | Human | Mouse | |||||
Entrez |
|
| |||||
Ensembl |
|
| |||||
UniProt |
|
| |||||
RefSeq (mRNA) |
|
| |||||
RefSeq (protein) |
|
| |||||
Location (UCSC) | n/a | n/a | |||||
PubMed search | n/a | n/a | |||||
Wikidata | |||||||
|
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
A number of selective ligands are available for NK3. NK3 receptor antagonists are being investigated as treatments for various indications.[3]
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
- Fezolinetant (ESN-364)
- MLE-4901 (also known as AZD-4901, formerly AZD-2624)
- Osanetant (SR-142,801)
- 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
- ↑ 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.
- ↑ 2.0 2.1 "Entrez Gene: TACR3 tachykinin receptor 3".
- ↑ 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
- Khawaja AM, Rogers DF (Jul 1996). "Tachykinins: receptor to effector". The International Journal of Biochemistry & Cell Biology. 28 (7): 721–38. doi:10.1016/1357-2725(96)00017-9. PMID 8925404.
- Advenier C, Lagente V, Boichot E (Aug 1997). "The role of tachykinin receptor antagonists in the prevention of bronchial hyperresponsiveness, airway inflammation and cough". The European Respiratory Journal. 10 (8): 1892–906. doi:10.1183/09031936.97.10081892. PMID 9272936.
- Buell G, Schulz MF, Arkinstall SJ, Maury K, Missotten M, Adami N, Talabot F, Kawashima E (Mar 1992). "Molecular characterisation, expression and localisation of human neurokinin-3 receptor". FEBS Letters. 299 (1): 90–5. doi:10.1016/0014-5793(92)80107-R. PMID 1312036.
- Takahashi K, Tanaka A, Hara M, Nakanishi S (Mar 1992). "The primary structure and gene organization of human substance P and neuromedin K receptors". European Journal of Biochemistry / FEBS. 204 (3): 1025–33. doi:10.1111/j.1432-1033.1992.tb16724.x. PMID 1312928.
- Xie GX, Miyajima A, Goldstein A (May 1992). "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. doi:10.1073/pnas.89.9.4124. PMC 525645. PMID 1315051.
- 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.
- Dion S, Corcos J, Carmel M, Drapeau G, Regoli D (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, Schmidt SK, Tucker JB, Brodbeck RM, Bu JY, Karpitskiy VV (Jan 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". Proceedings of the National Academy of Sciences of the United States of America. 94 (1): 310–5. doi:10.1073/pnas.94.1.310. PMC 19326. PMID 8990205.
- Brunelleschi S, Bordin G, Colangelo D, Viano I (Jun 1998). "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, Lomthaisong K, Gladwell RT, Butlin DJ, Manyonda IT, Lowry PJ (Jun 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, Cucchi P, Lecci A, Meini S, Patacchini R, Quartara L, Ricci R, Tramontana M, Giuliani S, Maggi CA (Jan 2002). "Pharmacological profile of the novel mammalian tachykinin, hemokinin 1". British Journal of Pharmacology. 135 (1): 266–74. doi:10.1038/sj.bjp.0704443. PMC 1573107. PMID 11786503.
- Graham GJ, Stevens JM, Page NM, Grant AD, Brain SD, Lowry PJ, Gibbins JM (Aug 2004). "Tachykinins regulate the function of platelets". Blood. 104 (4): 1058–65. doi:10.1182/blood-2003-11-3979. PMID 15130944.
- Page NM, Dakour J, Morrish DW (Jul 2006). "Gene regulation of neurokinin B and its receptor NK3 in late pregnancy and pre-eclampsia". Molecular Human Reproduction. 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.
This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it. |