Cholecystokinin A receptor

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Cholecystokinin A receptor
Protein CCKAR PDB 1d6g.png
PDB rendering based on 1d6g.
Available structures
PDB Ortholog search: PDBe, RCSB
Identifiers
Symbols CCKAR ; CCK-A; CCK1-R; CCK1R; CCKRA
External IDs OMIM118444 MGI99478 HomoloGene37337 IUPHAR: CCK1 ChEMBL: 1901 GeneCards: CCKAR Gene
RNA expression pattern
PBB GE CCKAR 211173 at tn.png
PBB GE CCKAR 211174 s at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 886 12425
Ensembl ENSG00000163394 ENSMUSG00000029193
UniProt P32238 O08786
RefSeq (mRNA) NM_000730 NM_009827
RefSeq (protein) NP_000721 NP_033957
Location (UCSC) Chr 4:
26.48 – 26.49 Mb
Chr 5:
53.7 – 53.71 Mb
PubMed search [1] [2]
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
Symbol CholecysA-Rec_N
Pfam PF09193
InterPro IPR015276
SCOP 1d6g
SUPERFAMILY 1d6g

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

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.[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[edit]

Agonists[edit]

  • 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[edit]

See also[edit]

References[edit]

  1. ^ "Entrez Gene: CCKAR cholecystokinin A receptor". 
  2. ^ Pellegrini M, Mierke DF (November 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[edit]

Further reading[edit]

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