Cholecystokinin receptor

Cholecystokinin receptors or CCK receptors are a group of G-protein coupled receptors which bind the peptide hormones cholecystokinin (CCK) and gastrin.[1] There are two different subtypes CCKA and CCKB which are ~50% homologous:[2] 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.

Protein Gene Tissue distribution Preferred ligand Function Mechanism
CCKA (CCK1) CCKAR primarily gastrointestinal tract, lesser amounts in the CNS sulfated CCK >> nonsulfated CCK ≈ nonsulfated CCK stimulation of bicarb secretion, gall bladder emptying and inhibiting gut motility Gq[3][4]
CCKB (CCK2) CCKBR primarily CNS, lesser amounts in the gastrointestinal tract gastrin ≈ CCK (receptor does not discriminate between sulfated and nonsulfated peptides) regulation of nociception, anxiety, memory and hunger Gq/G11[4]
cholecystokinin A receptor
Identifiers
SymbolCCKAR
NCBI gene886
HGNC1570
OMIM118444
RefSeqNM_000730
UniProtP32238
Other data
LocusChr. 4 p15.2-p15.1
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StructuresSwiss-model
DomainsInterPro
cholecystokinin B receptor
Identifiers
SymbolCCKBR
NCBI gene887
HGNC1571
OMIM118445
RefSeqNM_176875
UniProtP32239
Other data
LocusChr. 11 p15.4
Search for
StructuresSwiss-model
DomainsInterPro

References
  1. Noble F, Wank SA, Crawley JN, Bradwejn J, Seroogy KB, Hamon M, Roques BP (December 1999). "International Union of Pharmacology. XXI. Structure, distribution, and functions of cholecystokinin receptors". Pharmacological Reviews. 51 (4): 745–781. PMID 10581329.
  2. Dufresne M, Seva C, Fourmy D (July 2006). "Cholecystokinin and gastrin receptors". Physiological Reviews. 86 (3): 805–847. doi:10.1152/physrev.00014.2005. PMID 16816139.
  3. Wank SA (April 1998). "G protein-coupled receptors in gastrointestinal physiology. I. CCK receptors: an exemplary family". The American Journal of Physiology. 274 (4 Pt 1): G607–G613. doi:10.1152/ajpgi.1998.274.4.g607. PMID 9575840. S2CID 27674659.
  4. Beinfeld M, Chen Q, Gao F, Liddle RA, Miller LJ, Rehfeld J (2019-09-16). "Cholecystokinin receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database". IUPHAR/BPS Guide to Pharmacology CITE. 2019 (4). doi:10.2218/gtopdb/F15/2019.4. S2CID 203825385.
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