Tachykinin receptor 3: Difference between revisions

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{{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 ==


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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" />
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| update_protein_box = yes
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<!-- The GNF_Protein_box is automatically maintained by Protein Box Bot.  See Template:PBB_Controls to Stop updates. -->
== Selective ligands ==
{{GNF_Protein_box
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>
| image =
| image_source =
| PDB =  
| Name = Tachykinin receptor 3
| HGNCid = 11528
| Symbol = TACR3
| AltSymbols =; MGC148060; MGC148061; NK3R; TAC3RL
| OMIM = 162332
| ECnumber = 
| Homologene = 824
| MGIid = 892968
| GeneAtlas_image1 = PBB_GE_TACR3_208183_at_tn.png
| Function = {{GNF_GO|id=GO:0001584 |text = rhodopsin-like receptor activity}} {{GNF_GO|id=GO:0004872 |text = receptor activity}} {{GNF_GO|id=GO:0004995 |text = tachykinin receptor activity}}
| Component = {{GNF_GO|id=GO:0005886 |text = plasma membrane}} {{GNF_GO|id=GO:0005887 |text = integral to plasma membrane}}
| Process = {{GNF_GO|id=GO:0007165 |text = signal transduction}} {{GNF_GO|id=GO:0007217 |text = tachykinin signaling pathway}}
| Orthologs = {{GNF_Ortholog_box
    | Hs_EntrezGene = 6870
    | Hs_Ensembl = ENSG00000169836
    | Hs_RefseqProtein = NP_001050
    | Hs_RefseqmRNA = NM_001059
    | Hs_GenLoc_db = 
    | Hs_GenLoc_chr = 4
    | Hs_GenLoc_start = 104730074
    | Hs_GenLoc_end = 104860422
    | Hs_Uniprot = P29371
    | Mm_EntrezGene = 21338
    | Mm_Ensembl = ENSMUSG00000028172
    | Mm_RefseqmRNA = NM_021382
    | Mm_RefseqProtein = NP_067357
    | Mm_GenLoc_db =
    | Mm_GenLoc_chr = 3
    | Mm_GenLoc_start = 134766394
    | Mm_GenLoc_end = 134871959
    | Mm_Uniprot = Q6NXX1
  }}
}}
'''Tachykinin receptor 3''', also known as '''TACR3''', is a human [[gene]].<ref name="entrez">{{cite web | title = Entrez Gene: TACR3 tachykinin receptor 3| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=6870| accessdate = }}</ref>


<!-- The PBB_Summary template is automatically maintained by Protein Box Bot.  See Template:PBB_Controls to Stop updates. -->
=== Agonists ===
{{PBB_Summary
* [[Neurokinin B]] – endogenous peptide ligand, also interacts with other neurokinin receptors but has highest affinity for NK<sub>3</sub>
| section_title =  
* [[Senktide]] – 7-amino acid polypeptide, NK<sub>3</sub> selective, CAS# 106128-89-6
| summary_text = 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.<ref name="entrez">{{cite web | title = Entrez Gene: TACR3 tachykinin receptor 3| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=6870| accessdate = }}</ref>
}}


==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|2}}
{{reflist|35em}}


==Further reading==
== Further reading ==
{{refbegin | 2}}
{{refbegin|35em}}
{{PBB_Further_reading
* {{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 }}
| citations =
* {{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 | author=Khawaja AM, Rogers DF |title=Tachykinins: receptor to effector. |journal=Int. J. Biochem. Cell Biol. |volume=28 |issue= 7 |pages= 721-38 |year= 1996 |pmid= 8925404 |doi= }}
* {{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 | author=Advenier C, Lagente V, Boichot E |title=The role of tachykinin receptor antagonists in the prevention of bronchial hyperresponsiveness, airway inflammation and cough. |journal=Eur. Respir. J. |volume=10 |issue= 8 |pages= 1892-906 |year= 1997 |pmid= 9272936 |doi= }}
* {{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 | author=Buell G, Schulz MF, Arkinstall SJ, ''et al.'' |title=Molecular characterisation, expression and localisation of human neurokinin-3 receptor. |journal=FEBS Lett. |volume=299 |issue= 1 |pages= 90-5 |year= 1992 |pmid= 1312036 |doi= }}
* {{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 | author=Takahashi K, Tanaka A, Hara M, Nakanishi S |title=The primary structure and gene organization of human substance P and neuromedin K receptors. |journal=Eur. J. Biochem. |volume=204 |issue= 3 |pages= 1025-33 |year= 1992 |pmid= 1312928 |doi= }}
* {{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 | author=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=Proc. Natl. Acad. Sci. U.S.A. |volume=89 |issue= 9 |pages= 4124-8 |year= 1992 |pmid= 1315051 |doi= }}
* {{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 | author=Huang RR, Cheung AH, Mazina KE, ''et al.'' |title=cDNA sequence and heterologous expression of the human neurokinin-3 receptor. |journal=Biochem. Biophys. Res. Commun. |volume=184 |issue= 2 |pages= 966-72 |year= 1992 |pmid= 1374246 |doi= }}
* {{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 | author=Dion S, Corcos J, Carmel M, ''et al.'' |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= }}
* {{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 | author=Krause JE, Staveteig PT, Mentzer JN, ''et al.'' |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=Proc. Natl. Acad. Sci. U.S.A. |volume=94 |issue= 1 |pages= 310-5 |year= 1997 |pmid= 8990205 |doi= }}
* {{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 | author=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 |year= 1999 |pmid= 10189055 |doi= }}
* {{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 | author=Page NM, Woods RJ, Gardiner SM, ''et al.'' |title=Excessive placental secretion of neurokinin B during the third trimester causes pre-eclampsia. |journal=Nature |volume=405 |issue= 6788 |pages= 797-800 |year= 2000 |pmid= 10866201 |doi= 10.1038/35015579 }}
* {{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 | author=Bellucci F, Carini F, Catalani C, ''et al.'' |title=Pharmacological profile of the novel mammalian tachykinin, hemokinin 1. |journal=Br. J. Pharmacol. |volume=135 |issue= 1 |pages= 266-74 |year= 2002 |pmid= 11786503 |doi= 10.1038/sj.bjp.0704443 }}
* {{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 | author=Strausberg RL, Feingold EA, Grouse LH, ''et al.'' |title=Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=99 |issue= 26 |pages= 16899-903 |year= 2003 |pmid= 12477932 |doi= 10.1073/pnas.242603899 }}
*{{cite journal  | author=Graham GJ, Stevens JM, Page NM, ''et al.'' |title=Tachykinins regulate the function of platelets. |journal=Blood |volume=104 |issue= 4 |pages= 1058-65 |year= 2005 |pmid= 15130944 |doi= 10.1182/blood-2003-11-3979 }}
*{{cite journal | author=Gerhard DS, Wagner L, Feingold EA, ''et al.'' |title=The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). |journal=Genome Res. |volume=14 |issue= 10B |pages= 2121-7 |year= 2004 |pmid= 15489334 |doi= 10.1101/gr.2596504 }}
*{{cite journal  | author=Page NM, Dakour J, Morrish DW |title=Gene regulation of neurokinin B and its receptor NK3 in late pregnancy and pre-eclampsia. |journal=Mol. Hum. Reprod. |volume=12 |issue= 7 |pages= 427-33 |year= 2006 |pmid= 16709596 |doi= 10.1093/molehr/gal025 }}
}}
{{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]]


{{WH}}
 
{{WS}}
{{transmembranereceptor-stub}}

Revision as of 00:57, 27 October 2017

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Identifiers
Aliases
External IDsGeneCards: [1]
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

n/a

n/a

RefSeq (protein)

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Location (UCSC)n/an/a
PubMed searchn/an/a
Wikidata
View/Edit Human

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

  1. 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. 2.0 2.1 "Entrez Gene: TACR3 tachykinin receptor 3".
  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

External links

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