Cholecystokinin A receptor: Difference between revisions

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<!-- The PBB_Controls template provides controls for Protein Box Bot, please see Template:PBB_Controls for details. -->
{{Infobox_gene}}
{{PBB_Controls
{{Infobox protein family
| update_page = yes
| Symbol = CholecysA-Rec_N
| require_manual_inspection = no
| Name = Cholecystokinin A receptor, N-terminal domain
| update_protein_box = yes
| image = PDB 1d6g EBI.jpg
| update_summary = yes
| width =
| update_citations = yes
| caption = molecular complex of cholecystokinin-8 and n-terminus of the cholecystokinin a receptor by nmr spectroscopy
| Pfam = PF09193
| Pfam_clan = 
| InterPro = IPR015276
| SMART =
| PROSITE =
| MEROPS =
| SCOP = 1d6g
| TCDB =  
| OPM family =  
| OPM protein =  
| CAZy =  
| CDD =  
}}
}}
The '''Cholecystokinin A receptor''' is a human [[protein]], also known as '''CCKAR''' or '''CCK<sub>1</sub>''', with CCK<sub>1</sub> now being the [[IUPHAR]]-recommended name.


<!-- The GNF_Protein_box is automatically maintained by Protein Box Bot.  See Template:PBB_Controls to Stop updates. -->
== Function ==
{{GNF_Protein_box
 
| image = PBB_Protein_CCKAR_image.jpg
This gene encodes a G-protein coupled receptor that binds sulfated members of the cholecystokinin (CCK) family of peptide hormones. This receptor is a major physiologic mediator of pancreatic enzyme secretion and smooth muscle contraction of the gallbladder and stomach. In the central and peripheral nervous system this receptor regulates satiety and the release of beta-endorphin and dopamine.<ref name="entrez">{{cite web | title = Entrez Gene: CCKAR cholecystokinin A receptor| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=886| accessdate = }}</ref>
| image_source = [[Protein_Data_Bank|PDB]] rendering based on 1d6g.
 
| PDB = {{PDB2|1d6g}}
The extracellular, [[N-terminal]], [[protein domain|domain]] of this protein adopts a [[protein tertiary structure|tertiary structure]] consisting of a few [[Helix|helical]] [[turn (biochemistry)|turn]]s and a [[disulfide bond|disulfide]]-cross linked loop. It is required for interaction of the cholecystokinin A receptor with its corresponding [[Hormone|hormonal]] [[ligand (biochemistry)|ligand]].<ref name="pmid10555959">{{cite journal | vauthors = Pellegrini M, Mierke DF | title = Molecular complex of cholecystokinin-8 and N-terminus of the cholecystokinin A receptor by NMR spectroscopy | journal = Biochemistry | volume = 38 | issue = 45 | pages = 14775–83 | date = Nov 1999 | pmid = 10555959 | doi = 10.1021/bi991272l }}</ref>
| Name = Cholecystokinin A receptor
 
| HGNCid = 1570
==Selective Ligands==
| Symbol = CCKAR
 
| AltSymbols =; CCK-A; CCK1-R; CCKRA
===Agonists===
| OMIM = 118444
* [[Cholecystokinin]]
| ECnumber = 
* [[Gastrin]]
| Homologene = 37337
* [[CCK-4]]
| MGIid = 99478
* SR-146,131
| GeneAtlas_image1 = PBB_GE_CCKAR_211173_at_tn.png
* A-71623 - modified tetrapeptide, potent and selective CCK<sub>A</sub> agonist, IC<sub>50</sub> 3.7nM, 1200x selectivity over CCK<sub>B</sub>, CAS# 130408-77-4
| GeneAtlas_image2 = PBB_GE_CCKAR_211174_s_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:0004951 |text = cholecystokinin 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:0001764 |text = neuron migration}} {{GNF_GO|id=GO:0006939 |text = smooth muscle contraction}} {{GNF_GO|id=GO:0007165 |text = signal transduction}} {{GNF_GO|id=GO:0007200 |text = G-protein signaling, coupled to IP3 second messenger (phospholipase C activating)}} {{GNF_GO|id=GO:0007204 |text = elevation of cytosolic calcium ion concentration}} {{GNF_GO|id=GO:0007409 |text = axonogenesis}} {{GNF_GO|id=GO:0007584 |text = response to nutrient}} {{GNF_GO|id=GO:0007586 |text = digestion}} {{GNF_GO|id=GO:0007631 |text = feeding behavior}} {{GNF_GO|id=GO:0030900 |text = forebrain development}}  
| Orthologs = {{GNF_Ortholog_box
    | Hs_EntrezGene = 886
    | Hs_Ensembl = ENSG00000163394
    | Hs_RefseqProtein = NP_000721
    | Hs_RefseqmRNA = NM_000730
    | Hs_GenLoc_db = 
    | Hs_GenLoc_chr = 4
    | Hs_GenLoc_start = 26092116
    | Hs_GenLoc_end = 26101140
    | Hs_Uniprot = P32238
    | Mm_EntrezGene = 12425
    | Mm_Ensembl = ENSMUSG00000029193
    | Mm_RefseqmRNA = NM_009827
    | Mm_RefseqProtein = NP_033957
    | Mm_GenLoc_db = 
    | Mm_GenLoc_chr = 5
    | Mm_GenLoc_start = 53986735
    | Mm_GenLoc_end = 53996350
    | Mm_Uniprot = Q3TPL0
  }}
}}
'''Cholecystokinin A receptor''', also known as '''CCKAR''', is a human [[gene]].


<!-- The PBB_Summary template is automatically maintained by Protein Box Bot.  See Template:PBB_Controls to Stop updates. -->
===Antagonists===
{{PBB_Summary
* [[Proglumide]]
| section_title =  
* [[Lorglumide]]
| summary_text = This gene encodes a G-protein coupled receptor that binds non-sulfated members of the cholecystokinin (CCK) family of peptide hormones. This receptor is a major physiologic mediator of pancreatic enzyme secretion and smooth muscle contraction of the gallbladder and stomach. In the central and peripheral nervous system this receptor regulates satiety and the release of beta-endorphin and dopamine.<ref name="entrez">{{cite web | title = Entrez Gene: CCKAR cholecystokinin A receptor| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=886| accessdate = }}</ref>
* [[Devazepide]]
}}
* [[Dexloxiglumide]]
* [[Asperlicin]]
* SR-27897
* IQM-95333
* JNJ-17156516


==See also==
== See also ==
* [[Cholecystokinin receptor]]
* [[Cholecystokinin receptor]]
* [[Cholecystokinin antagonist]]
* [[Cholecystokinin antagonist]]


==References==
== References ==
{{reflist|2}}
{{reflist}}


==Further reading==
== External links ==
* {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2247 | title = Cholecystokinin Receptors: CCK<sub>1</sub> | accessdate = | authorlink = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | archiveurl = | archivedate = | quote = }}
 
== Further reading ==
{{refbegin | 2}}
{{refbegin | 2}}
{{PBB_Further_reading
* {{cite journal | vauthors = Varga G, Bálint A, Burghardt B, D'Amato M | title = Involvement of endogenous CCK and CCK1 receptors in colonic motor function | journal = British Journal of Pharmacology | volume = 141 | issue = 8 | pages = 1275–84 | date = Apr 2004 | pmid = 15100163 | pmc = 1574909 | doi = 10.1038/sj.bjp.0705769 }}
| citations =
* {{cite journal | vauthors = Wang J, Si YM, Liu ZL, Yu L | title = Cholecystokinin, cholecystokinin-A receptor and cholecystokinin-B receptor gene polymorphisms in Parkinson's disease | journal = Pharmacogenetics | volume = 13 | issue = 6 | pages = 365–9 | date = Jun 2003 | pmid = 12777967 | doi = 10.1097/00008571-200306000-00008 }}
*{{cite journal | author=Varga G, Bálint A, Burghardt B, D'Amato M |title=Involvement of endogenous CCK and CCK1 receptors in colonic motor function. |journal=Br. J. Pharmacol. |volume=141 |issue= 8 |pages= 1275-84 |year= 2004 |pmid= 15100163 |doi= 10.1038/sj.bjp.0705769 }}
* {{cite journal | vauthors = Miller LJ, Holicky EL, Ulrich CD, Wieben ED | title = Abnormal processing of the human cholecystokinin receptor gene in association with gallstones and obesity | journal = Gastroenterology | volume = 109 | issue = 4 | pages = 1375–80 | date = Oct 1995 | pmid = 7557108 | doi = 10.1016/0016-5085(95)90601-0 }}
*{{cite journal | author=Miller LJ, Holicky EL, Ulrich CD, Wieben ED |title=Abnormal processing of the human cholecystokinin receptor gene in association with gallstones and obesity. |journal=Gastroenterology |volume=109 |issue= 4 |pages= 1375-80 |year= 1995 |pmid= 7557108 |doi= }}
* {{cite journal | vauthors = Huppi K, Siwarski D, Pisegna JR, Wank S | title = Chromosomal localization of the gastric and brain receptors for cholecystokinin (CCKAR and CCKBR) in human and mouse | journal = Genomics | volume = 25 | issue = 3 | pages = 727–9 | date = Feb 1995 | pmid = 7759110 | doi = 10.1016/0888-7543(95)80018-H }}
*{{cite journal | author=Huppi K, Siwarski D, Pisegna JR, Wank S |title=Chromosomal localization of the gastric and brain receptors for cholecystokinin (CCKAR and CCKBR) in human and mouse. |journal=Genomics |volume=25 |issue= 3 |pages= 727-9 |year= 1995 |pmid= 7759110 |doi= }}
* {{cite journal | vauthors = de Weerth A, Pisegna JR, Huppi K, Wank SA | title = Molecular cloning, functional expression and chromosomal localization of the human cholecystokinin type A receptor | journal = Biochemical and Biophysical Research Communications | volume = 194 | issue = 2 | pages = 811–8 | date = Jul 1993 | pmid = 8343165 | doi = 10.1006/bbrc.1993.1894 }}
*{{cite journal | author=de Weerth A, Pisegna JR, Huppi K, Wank SA |title=Molecular cloning, functional expression and chromosomal localization of the human cholecystokinin type A receptor. |journal=Biochem. Biophys. Res. Commun. |volume=194 |issue= 2 |pages= 811-8 |year= 1993 |pmid= 8343165 |doi= }}
* {{cite journal | vauthors = Ulrich CD, Ferber I, Holicky E, Hadac E, Buell G, Miller LJ | title = Molecular cloning and functional expression of the human gallbladder cholecystokinin A receptor | journal = Biochemical and Biophysical Research Communications | volume = 193 | issue = 1 | pages = 204–11 | date = May 1993 | pmid = 8503909 | doi = 10.1006/bbrc.1993.1610 }}
*{{cite journal | author=Ulrich CD, Ferber I, Holicky E, ''et al.'' |title=Molecular cloning and functional expression of the human gallbladder cholecystokinin A receptor. |journal=Biochem. Biophys. Res. Commun. |volume=193 |issue= 1 |pages= 204-11 |year= 1993 |pmid= 8503909 |doi= 10.1006/bbrc.1993.1610 }}
* {{cite journal | vauthors = Kennedy K, Gigoux V, Escrieut C, Maigret B, Martinez J, Moroder L, Fréhel D, Gully D, Vaysse N, Fourmy D | title = Identification of two amino acids of the human cholecystokinin-A receptor that interact with the N-terminal moiety of cholecystokinin | journal = The Journal of Biological Chemistry | volume = 272 | issue = 5 | pages = 2920–6 | date = Jan 1997 | pmid = 9006937 | doi = 10.1074/jbc.272.5.2920 }}
*{{cite journal | author=Kennedy K, Gigoux V, Escrieut C, ''et al.'' |title=Identification of two amino acids of the human cholecystokinin-A receptor that interact with the N-terminal moiety of cholecystokinin. |journal=J. Biol. Chem. |volume=272 |issue= 5 |pages= 2920-6 |year= 1997 |pmid= 9006937 |doi= }}
* {{cite journal | vauthors = Inoue H, Iannotti CA, Welling CM, Veile R, Donis-Keller H, Permutt MA | title = Human cholecystokinin type A receptor gene: cytogenetic localization, physical mapping, and identification of two missense variants in patients with obesity and non-insulin-dependent diabetes mellitus (NIDDM) | journal = Genomics | volume = 42 | issue = 2 | pages = 331–5 | date = Jun 1997 | pmid = 9192855 | doi = 10.1006/geno.1997.4749 }}
*{{cite journal | author=Inoue H, Iannotti CA, Welling CM, ''et al.'' |title=Human cholecystokinin type A receptor gene: cytogenetic localization, physical mapping, and identification of two missense variants in patients with obesity and non-insulin-dependent diabetes mellitus (NIDDM). |journal=Genomics |volume=42 |issue= 2 |pages= 331-5 |year= 1997 |pmid= 9192855 |doi= 10.1006/geno.1997.4749 }}
* {{cite journal | vauthors = Gigoux V, Escrieut C, Silvente-Poirot S, Maigret B, Gouilleux L, Fehrentz JA, Gully D, Moroder L, Vaysse N, Fourmy D | title = Met-195 of the cholecystokinin-A receptor interacts with the sulfated tyrosine of cholecystokinin and is crucial for receptor transition to high affinity state | journal = The Journal of Biological Chemistry | volume = 273 | issue = 23 | pages = 14380–6 | date = Jun 1998 | pmid = 9603948 | doi = 10.1074/jbc.273.23.14380 }}
*{{cite journal | author=Gigoux V, Escrieut C, Silvente-Poirot S, ''et al.'' |title=Met-195 of the cholecystokinin-A receptor interacts with the sulfated tyrosine of cholecystokinin and is crucial for receptor transition to high affinity state. |journal=J. Biol. Chem. |volume=273 |issue= 23 |pages= 14380-6 |year= 1998 |pmid= 9603948 |doi= }}
* {{cite journal | vauthors = Funakoshi A, Fukamizu Y, Miyasaka K | title = Mechanism of cholecystokinin-A- receptor antagonist on human pancreatic exocrine secretion. Localization of CCK-A receptor in the human duodenum | journal = Digestion | volume = 60 Suppl 1 | issue = | pages = 75–80 | year = 2000 | pmid = 10026437 | doi = 10.1159/000051459 }}
*{{cite journal | author=Funakoshi A, Fukamizu Y, Miyasaka K |title=Mechanism of cholecystokinin-A- receptor antagonist on human pancreatic exocrine secretion. Localization of CCK-A receptor in the human duodenum. |journal=Digestion |volume=60 Suppl 1 |issue= |pages= 75-80 |year= 2000 |pmid= 10026437 |doi= }}
* {{cite journal | vauthors = Gigoux V, Escrieut C, Fehrentz JA, Poirot S, Maigret B, Moroder L, Gully D, Martinez J, Vaysse N, Fourmy D | title = Arginine 336 and asparagine 333 of the human cholecystokinin-A receptor binding site interact with the penultimate aspartic acid and the C-terminal amide of cholecystokinin | journal = The Journal of Biological Chemistry | volume = 274 | issue = 29 | pages = 20457–64 | date = Jul 1999 | pmid = 10400673 | doi = 10.1074/jbc.274.29.20457 }}
*{{cite journal | author=Gigoux V, Escrieut C, Fehrentz JA, ''et al.'' |title=Arginine 336 and asparagine 333 of the human cholecystokinin-A receptor binding site interact with the penultimate aspartic acid and the C-terminal amide of cholecystokinin. |journal=J. Biol. Chem. |volume=274 |issue= 29 |pages= 20457-64 |year= 1999 |pmid= 10400673 |doi= }}
* {{cite journal | vauthors = Gigoux V, Maigret B, Escrieut C, Silvente-Poirot S, Bouisson M, Fehrentz JA, Moroder L, Gully D, Martinez J, Vaysse N, Fourmy AD | title = Arginine 197 of the cholecystokinin-A receptor binding site interacts with the sulfate of the peptide agonist cholecystokinin | journal = Protein Science | volume = 8 | issue = 11 | pages = 2347–54 | date = Nov 1999 | pmid = 10595537 | pmc = 2144185 | doi = 10.1110/ps.8.11.2347 }}
*{{cite journal | author=Pellegrini M, Mierke DF |title=Molecular complex of cholecystokinin-8 and N-terminus of the cholecystokinin A receptor by NMR spectroscopy. |journal=Biochemistry |volume=38 |issue= 45 |pages= 14775-83 |year= 1999 |pmid= 10555959 |doi= }}
* {{cite journal | vauthors = Funakoshi A, Miyasaka K, Matsumoto H, Yamamori S, Takiguchi S, Kataoka K, Takata Y, Matsusue K, Kono A, Shimokata H | title = Gene structure of human cholecystokinin (CCK) type-A receptor: body fat content is related to CCK type-A receptor gene promoter polymorphism | journal = FEBS Letters | volume = 466 | issue = 2-3 | pages = 264–6 | date = Jan 2000 | pmid = 10682840 | doi = 10.1016/S0014-5793(00)01080-2 }}
*{{cite journal | author=Gigoux V, Maigret B, Escrieut C, ''et al.'' |title=Arginine 197 of the cholecystokinin-A receptor binding site interacts with the sulfate of the peptide agonist cholecystokinin. |journal=Protein Sci. |volume=8 |issue= 11 |pages= 2347-54 |year= 2000 |pmid= 10595537 |doi= }}
* {{cite journal | vauthors = Tachikawa H, Harada S, Kawanishi Y, Okubo T, Shiraishi H | title = Novel polymorphisms of the human cholecystokinin A receptor gene: an association analysis with schizophrenia | journal = American Journal of Medical Genetics | volume = 96 | issue = 2 | pages = 141–5 | date = Apr 2000 | pmid = 10893485 | doi = 10.1002/(SICI)1096-8628(20000403)96:2<141::AID-AJMG3>3.0.CO;2-R }}
*{{cite journal | author=Funakoshi A, Miyasaka K, Matsumoto H, ''et al.'' |title=Gene structure of human cholecystokinin (CCK) type-A receptor: body fat content is related to CCK type-A receptor gene promoter polymorphism. |journal=FEBS Lett. |volume=466 |issue= 2-3 |pages= 264-6 |year= 2000 |pmid= 10682840 |doi= }}
* {{cite journal | vauthors = Giragossian C, Mierke DF | title = Intermolecular interactions between cholecystokinin-8 and the third extracellular loop of the cholecystokinin A receptor | journal = Biochemistry | volume = 40 | issue = 13 | pages = 3804–9 | date = Apr 2001 | pmid = 11300760 | doi = 10.1021/bi002659n }}
*{{cite journal | author=Tachikawa H, Harada S, Kawanishi Y, ''et al.'' |title=Novel polymorphisms of the human cholecystokinin A receptor gene: an association analysis with schizophrenia. |journal=Am. J. Med. Genet. |volume=96 |issue= 2 |pages= 141-5 |year= 2000 |pmid= 10893485 |doi= }}
* {{cite journal | vauthors = Schmitz F, Schrader H, Otte J, Schmitz H, Stüber E, Herzig K, Schmidt WE | title = Identification of CCK-B/gastrin receptor splice variants in human peripheral blood mononuclear cells | journal = Regulatory Peptides | volume = 101 | issue = 1-3 | pages = 25–33 | date = Sep 2001 | pmid = 11495676 | doi = 10.1016/S0167-0115(01)00281-6 }}
*{{cite journal  | author=Giragossian C, Mierke DF |title=Intermolecular interactions between cholecystokinin-8 and the third extracellular loop of the cholecystokinin A receptor. |journal=Biochemistry |volume=40 |issue= 13 |pages= 3804-9 |year= 2001 |pmid= 11300760 |doi= }}
* {{cite journal | vauthors = Tachikawa H, Harada S, Kawanishi Y, Okubo T, Suzuki T | title = Linked polymorphisms (-333G>T and -286A>G) in the promoter region of the CCK-A receptor gene may be associated with schizophrenia | journal = Psychiatry Research | volume = 103 | issue = 2-3 | pages = 147–55 | date = Sep 2001 | pmid = 11549403 | doi = 10.1016/S0165-1781(01)00276-1 }}
*{{cite journal | author=Schmitz F, Schrader H, Otte J, ''et al.'' |title=Identification of CCK-B/gastrin receptor splice variants in human peripheral blood mononuclear cells. |journal=Regul. Pept. |volume=101 |issue= 1-3 |pages= 25-33 |year= 2002 |pmid= 11495676 |doi= }}
* {{cite journal | vauthors = Schmitz F, Göke MN, Otte JM, Schrader H, Reimann B, Kruse ML, Siegel EG, Peters J, Herzig KH, Fölsch UR, Schmidt WE | title = Cellular expression of CCK-A and CCK-B/gastrin receptors in human gastric mucosa | journal = Regulatory Peptides | volume = 102 | issue = 2-3 | pages = 101–10 | date = Dec 2001 | pmid = 11730982 | doi = 10.1016/S0167-0115(01)00307-X }}
*{{cite journal | author=Tachikawa H, Harada S, Kawanishi Y, ''et al.'' |title=Linked polymorphisms (-333G>T and -286A>G) in the promoter region of the CCK-A receptor gene may be associated with schizophrenia. |journal=Psychiatry research |volume=103 |issue= 2-3 |pages= 147-55 |year= 2002 |pmid= 11549403 |doi= }}
* {{cite journal | vauthors = Okubo T, Harada S, Higuchi S, Matsushita S | title = Investigation of quantitative trait loci in the CCKAR gene with susceptibility to alcoholism | journal = Alcoholism, Clinical and Experimental Research | volume = 26 | issue = 8 Suppl | pages = 2S-5S | date = Aug 2002 | pmid = 12198366 | doi = 10.1097/01.ALC.0000026826.96191.FB }}
*{{cite journal | author=Schmitz F, Göke MN, Otte JM, ''et al.'' |title=Cellular expression of CCK-A and CCK-B/gastrin receptors in human gastric mucosa. |journal=Regul. Pept. |volume=102 |issue= 2-3 |pages= 101-10 |year= 2002 |pmid= 11730982 |doi= }}
* {{cite journal | vauthors = Takata Y, Takeda S, Kawanami T, Takiguchi S, Yoshida Y, Miyasaka K, Funakoshi A | title = Promoter analysis of human cholecystokinin type-A receptor gene | journal = Journal of Gastroenterology | volume = 37 | issue = 10 | pages = 815–20 | year = 2003 | pmid = 12424565 | doi = 10.1007/s005350200135 }}
*{{cite journal | author=Okubo T, Harada S, Higuchi S, Matsushita S |title=Investigation of quantitative trait loci in the CCKAR gene with susceptibility to alcoholism. |journal=Alcohol. Clin. Exp. Res. |volume=26 |issue= 8 Suppl |pages= 2S-5S |year= 2003 |pmid= 12198366 |doi= 10.1097/01.ALC.0000026826.96191.FB }}
*{{cite journal | author=Takata Y, Takeda S, Kawanami T, ''et al.'' |title=Promoter analysis of human cholecystokinin type-A receptor gene. |journal=J. Gastroenterol. |volume=37 |issue= 10 |pages= 815-20 |year= 2003 |pmid= 12424565 |doi= 10.1007/s005350200135 }}
}}
{{refend}}
{{refend}}


{{NLM content}}
{{NLM content}}
{{membrane-protein-stub}}
 
{{PDB Gallery|geneid=886}}
{{G protein-coupled receptors}}
{{G protein-coupled receptors}}
{{Neuropeptide receptors}}
{{Neuropeptide receptors}}
[[Category:G protein coupled receptors]]
{{Neuropeptidergics}}
 
{{InterPro content|IPR015276}}
 
[[Category:G protein-coupled receptors]]
[[Category:Protein domains]]
[[Category:Cholecystokinin receptors]]

Latest revision as of 12:00, 10 January 2019

VALUE_ERROR (nil)
Identifiers
Aliases
External IDsGeneCards: [1]
Orthologs
SpeciesHumanMouse
Entrez

n/a

n/a

Ensembl

n/a

n/a

UniProt

n/a

n/a

RefSeq (mRNA)

n/a

n/a

RefSeq (protein)

n/a

n/a

Location (UCSC)n/an/a
PubMed searchn/an/a
Wikidata
View/Edit Human
Cholecystokinin A receptor, N-terminal domain
File:PDB 1d6g EBI.jpg
molecular complex of cholecystokinin-8 and n-terminus of the cholecystokinin a receptor by nmr spectroscopy
Identifiers
SymbolCholecysA-Rec_N
PfamPF09193
InterProIPR015276
SCOP1d6g
SUPERFAMILY1d6g

The Cholecystokinin A receptor is a human protein, also known as CCKAR or CCK1, with CCK1 now being the IUPHAR-recommended name.

Function

This gene encodes a G-protein coupled receptor that binds sulfated members of the cholecystokinin (CCK) family of peptide hormones. This receptor is a major physiologic mediator of pancreatic enzyme secretion and smooth muscle contraction of the gallbladder and stomach. In the central and peripheral nervous system this receptor regulates satiety and the release of beta-endorphin and dopamine.[1]

The extracellular, N-terminal, domain of this protein adopts a tertiary structure consisting of a few helical turns and a disulfide-cross linked loop. It is required for interaction of the cholecystokinin A receptor with its corresponding hormonal ligand.[2]

Selective Ligands

Agonists

  • Cholecystokinin
  • Gastrin
  • CCK-4
  • SR-146,131
  • A-71623 - modified tetrapeptide, potent and selective CCKA agonist, IC50 3.7nM, 1200x selectivity over CCKB, CAS# 130408-77-4

Antagonists

See also

References

  1. ↑ "Entrez Gene: CCKAR cholecystokinin A receptor".
  2. ↑ Pellegrini M, Mierke DF (Nov 1999). "Molecular complex of cholecystokinin-8 and N-terminus of the cholecystokinin A receptor by NMR spectroscopy". Biochemistry. 38 (45): 14775–83. doi:10.1021/bi991272l. PMID 10555959.

External links

Further reading

  • Varga G, Bálint A, Burghardt B, D'Amato M (Apr 2004). "Involvement of endogenous CCK and CCK1 receptors in colonic motor function". British Journal of Pharmacology. 141 (8): 1275–84. doi:10.1038/sj.bjp.0705769. PMC 1574909. PMID 15100163.
  • Wang J, Si YM, Liu ZL, Yu L (Jun 2003). "Cholecystokinin, cholecystokinin-A receptor and cholecystokinin-B receptor gene polymorphisms in Parkinson's disease". Pharmacogenetics. 13 (6): 365–9. doi:10.1097/00008571-200306000-00008. PMID 12777967.
  • Miller LJ, Holicky EL, Ulrich CD, Wieben ED (Oct 1995). "Abnormal processing of the human cholecystokinin receptor gene in association with gallstones and obesity". Gastroenterology. 109 (4): 1375–80. doi:10.1016/0016-5085(95)90601-0. PMID 7557108.
  • Huppi K, Siwarski D, Pisegna JR, Wank S (Feb 1995). "Chromosomal localization of the gastric and brain receptors for cholecystokinin (CCKAR and CCKBR) in human and mouse". Genomics. 25 (3): 727–9. doi:10.1016/0888-7543(95)80018-H. PMID 7759110.
  • de Weerth A, Pisegna JR, Huppi K, Wank SA (Jul 1993). "Molecular cloning, functional expression and chromosomal localization of the human cholecystokinin type A receptor". Biochemical and Biophysical Research Communications. 194 (2): 811–8. doi:10.1006/bbrc.1993.1894. PMID 8343165.
  • Ulrich CD, Ferber I, Holicky E, Hadac E, Buell G, Miller LJ (May 1993). "Molecular cloning and functional expression of the human gallbladder cholecystokinin A receptor". Biochemical and Biophysical Research Communications. 193 (1): 204–11. doi:10.1006/bbrc.1993.1610. PMID 8503909.
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This article incorporates text from the United States National Library of Medicine, which is in the public domain.



This article incorporates text from the public domain Pfam and InterPro: IPR015276
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