Cholecystokinin A receptor

Last updated
CCKAR
Protein CCKAR PDB 1d6g.png
Available structures
PDB Ortholog search: PDBe RCSB
Identifiers
Aliases CCKAR , CCK-A, CCK1-R, CCK1R, CCKRA, cholecystokinin A receptor
External IDs OMIM: 118444 MGI: 99478 HomoloGene: 37337 GeneCards: CCKAR
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_000730

NM_009827
NM_001347354

RefSeq (protein)

NP_000721

NP_001334283
NP_033957

Location (UCSC) Chr 4: 26.48 – 26.49 Mb Chr 5: 53.86 – 53.87 Mb
PubMed search [3] [4]
Wikidata
View/Edit Human View/Edit Mouse
Cholecystokinin A receptor, N-terminal domain
PDB 1d6g EBI.jpg
molecular complex of cholecystokinin-8 and n-terminus of the cholecystokinin a receptor by nmr spectroscopy
Identifiers
SymbolCholecysA-Rec_N
Pfam PF09193
InterPro IPR015276
SCOP2 1d6g / SCOPe / SUPFAM
Available protein structures:
Pfam   structures / ECOD  
PDB RCSB PDB; PDBe; PDBj
PDBsum structure summary

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

Contents

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. [5]

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. [6]

Selective Ligands

Agonists

Antagonists

See also

Related Research Articles

<span class="mw-page-title-main">Cholecystokinin</span> Hormone of the gastrointestinal system

Cholecystokinin is a peptide hormone of the gastrointestinal system responsible for stimulating the digestion of fat and protein. Cholecystokinin, formerly called pancreozymin, is synthesized and secreted by enteroendocrine cells in the duodenum, the first segment of the small intestine. Its presence causes the release of digestive enzymes and bile from the pancreas and gallbladder, respectively, and also acts as a hunger suppressant.

<span class="mw-page-title-main">Gastrin</span> Mammalian protein found in Homo sapiens

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Cholecystokinin receptors or CCK receptors are a group of G-protein coupled receptors which bind the peptide hormones cholecystokinin (CCK) and gastrin. There are two different subtypes CCKA and CCKB which are ~50% homologous: Various cholecystokinin antagonists have been developed and are used in research, although the only drug of this class that has been widely marketed to date is the anti-ulcer drug proglumide.

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The prolactin-releasing peptide receptor (PrRPR) also known as G-protein coupled receptor 10 (GPR10) is a protein that in humans is encoded by the PRLHR gene.

<span class="mw-page-title-main">Cholecystokinin B receptor</span> Protein-coding gene in the species Homo sapiens

The cholecystokinin B receptor also known as CCKBR or CCK2 is a protein that in humans is encoded by the CCKBR gene.

<span class="mw-page-title-main">Natriuretic peptide precursor C</span> Protein-coding gene in the species Homo sapiens

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<span class="mw-page-title-main">Neuropeptide Y receptor Y5</span> Protein-coding gene in the species Homo sapiens

Neuropeptide Y receptor type 5 is a protein that in humans is encoded by the NPY5R gene.

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Galanin receptor 3 (GAL3) is a G-protein coupled receptor encoded by the GALR3 gene.

<span class="mw-page-title-main">Neurotensin receptor 1</span> Protein-coding gene in the species Homo sapiens

Neurotensin receptor type 1 is a protein that in humans is encoded by the NTSR1 gene. For a crystal structure of NTS1, see pdb code 4GRV. In addition, high-resolution crystal structures have been determined in complex with the peptide full agonist NTS8-13, the non-peptide full agonist SRI-9829, the partial agonist RTI-3a, and the antagonists / inverse agonists SR48692 and SR142948A, as well as in the ligand-free apo state., see PDB codes 6YVR (NTSR1-H4X:NTS8–13), 6Z4V (NTSR1-H4bmX:NTS8–13), 6Z8N (NTSR1-H4X:SRI-9829), 6ZA8 (NTSR1-H4X:RTI-3a), 6Z4S (NTSR1-H4bmX:SR48692), 6ZIN (NTSR1-H4X:SR48692), 6Z4Q, and 6Z66.

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<span class="mw-page-title-main">PRKD2</span> Protein-coding gene in the species Homo sapiens

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<span class="mw-page-title-main">Neuropeptide FF</span> Protein-coding gene in the species Homo sapiens

NPFF Neuropeptide FF (FLFQPQRFa) is a mammalian amidated neuropeptide originally isolated from bovine brain and characterized as a pain-modulating peptide, with anti-opioid activity on morphine-induced analgesia.

<span class="mw-page-title-main">CCK-4</span> Anxiogenic agent

Cholecystokinin tetrapeptide (CCK-4, tetragastrin, Trp-Met-Asp-Phe-NH2) is a peptide fragment derived from the larger peptide hormone cholecystokinin. Unlike cholecystokin which has a variety of roles in the gastrointestinal system as well as central nervous system effects, CCK-4 acts primarily in the brain as an anxiogenic, although it does retain some GI effects, but not as much as CCK-8 or the full length polypeptide CCK-58.

<span class="mw-page-title-main">Monitor peptide</span>

Monitor peptide, also known as pancreatic secretory trypsin inhibitor I (PSTI-I) or pancreatic secretory trypsin inhibitor 61 (PSTI-61), is a peptide that plays an important role in the regulation of the digestive system, specifically the release of cholecystokinin (CCK).

References

  1. 1 2 3 GRCh38: Ensembl release 89: ENSG00000163394 - Ensembl, May 2017
  2. 1 2 3 GRCm38: Ensembl release 89: ENSMUSG00000029193 - Ensembl, May 2017
  3. "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. "Entrez Gene: CCKAR cholecystokinin A receptor".
  6. 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.

Further reading

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