Cholecystokinin receptor explained

cholecystokinin A receptor
Hgncid:1570
Symbol:CCKAR
Entrezgene:886
Omim:118444
Refseq:NM_000730
Uniprot:P32238
Chromosome:4
Arm:p
Band:15.2
Locussupplementarydata:-p15.1
cholecystokinin B receptor
Hgncid:1571
Symbol:CCKBR
Entrezgene:887
Omim:118445
Refseq:NM_176875
Uniprot:P32239
Chromosome:11
Arm:p
Band:15.4

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.

ProteinGeneTissue distributionPreferred ligandFunctionMechanism
CCKA (CCK1)primarily gastrointestinal tract, lesser amounts in the CNSsulfated CCK >> nonsulfated CCK ≈ nonsulfated CCKstimulation of bicarb secretion, gall bladder emptying and inhibiting gut motilityGq[3] [4]
CCKB (CCK2)primarily CNS, lesser amounts in the gastrointestinal tractgastrin ≈ CCK (receptor does not discriminate between sulfated and nonsulfated peptides)regulation of nociception, anxiety, memory and hungerGq/G11

Notes and References

  1. Noble F, Wank SA, Crawley JN, Bradwejn J, Seroogy KB, Hamon M, Roques BP . International Union of Pharmacology. XXI. Structure, distribution, and functions of cholecystokinin receptors . Pharmacological Reviews . 51 . 4 . 745–781 . December 1999 . 10581329 . Jacqueline Crawley .
  2. Dufresne M, Seva C, Fourmy D . Cholecystokinin and gastrin receptors . Physiological Reviews . 86 . 3 . 805–847 . July 2006 . 16816139 . 10.1152/physrev.00014.2005 .
  3. Wank SA . G protein-coupled receptors in gastrointestinal physiology. I. CCK receptors: an exemplary family . The American Journal of Physiology . 274 . 4 Pt 1 . G607–G613 . April 1998 . 9575840 . 10.1152/ajpgi.1998.274.4.g607 . 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 . en . 2019 . 4 . 10.2218/gtopdb/F15/2019.4 . 203825385 . free .