Cholecystokinin A receptor

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

CCKAR
Available structures PDB Ortholog search: PDBe RCSB List of PDB id codes 1D6G, 1HZN
Identifiers
Aliases	CCKAR, CCK-A, CCK1-R, CCK1R, CCKRA, cholecystokinin A receptor
External IDs	OMIM: 118444; MGI: 99478; HomoloGene: 37337; GeneCards: CCKAR; OMA:CCKAR - orthologs
Gene location (Human) Chr. Chromosome 4 (human)[1] Band 4p15.2 Start 26,481,396 bp[1] End 26,490,484 bp[1]
Gene location (Mouse) Chr. Chromosome 5 (mouse)[2] Band 5 C1|5 29.52 cM Start 53,855,118 bp[2] End 53,865,047 bp[2]
RNA expression pattern Bgee Human Mouse (ortholog) Top expressed in gallbladder body of stomach fundus embryo islet of Langerhans duodenum ganglionic eminence hypothalamus sensory organ tonsil Top expressed in epithelium of stomach right lung lobe lumbar spinal ganglion right kidney proximal tubule pyloric antrum human kidney left lung left lung lobe thyroid gland More reference expression data BioGPS More reference expression data
Gene ontology Molecular function G protein-coupled receptor activity signal transducer activity peptide binding cholecystokinin receptor activity peptide hormone binding Cellular component integral component of membrane plasma membrane integral component of plasma membrane membrane Biological process axonogenesis neuron migration phospholipase C-activating G protein-coupled receptor signaling pathway forebrain development signal transduction regulation of hormone secretion cellular response to hormone stimulus response to peptide G protein-coupled receptor signaling pathway cholecystokinin signaling pathway feeding behavior Sources:Amigo / QuickGO
Orthologs Species Human Mouse Entrez 886 12425 Ensembl ENSG00000163394 ENSMUSG00000029193 UniProt P32238 O08786 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
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Cholecystokinin A receptor, N-terminal domain
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
SCOP2	1d6g / SCOPe / SUPFAM
Available protein structures: Pfam   structures / ECOD   PDB RCSB PDB; PDBe; PDBj PDBsum structure summary

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

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

Antagonists

• Proglumide
• Lorglumide
• Devazepide
• Dexloxiglumide
• Asperlicin
• SR-27897
• IQM-95333
• JNJ-17156516

See also

• Cholecystokinin receptor
• Cholecystokinin antagonist