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Cholecystokinin A receptor

From Wikipedia, the free encyclopedia

CCKAR
Available structures
PDBOrtholog search: PDBe RCSB
Identifiers
AliasesCCKAR, CCK-A, CCK1-R, CCK1R, CCKRA, cholecystokinin A receptor
External IDsOMIM: 118444; MGI: 99478; HomoloGene: 37337; GeneCards: CCKAR; OMA:CCKAR - orthologs
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 MbChr 5: 53.86 – 53.87 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse
Cholecystokinin A receptor, N-terminal domain
molecular complex of cholecystokinin-8 and n-terminus of the cholecystokinin a receptor by nmr spectroscopy
Identifiers
SymbolCholecysA-Rec_N
PfamPF09193
InterProIPR015276
SCOP21d6g / SCOPe / SUPFAM
Available protein structures:
Pfam  structures / ECOD  
PDBRCSB PDB; PDBe; PDBj
PDBsumstructure summary

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

Function

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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

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Agonists

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  • Cholecystokinin
  • 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

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See also

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References

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  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000163394Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000029193Ensembl, 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.
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Further reading

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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