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.
Protein | Gene | Tissue distribution | Preferred ligand | Function | Mechanism |
---|
CCKA (CCK1) | | 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) | | 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 | |
Notes and References
- 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 .
- Dufresne M, Seva C, Fourmy D . Cholecystokinin and gastrin receptors . Physiological Reviews . 86 . 3 . 805–847 . July 2006 . 16816139 . 10.1152/physrev.00014.2005 .
- 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 .
- 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 .