Biology:Cholecystokinin receptor

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Short description: G-protein coupled receptor
cholecystokinin A receptor
Identifiers
SymbolCCKAR
NCBI gene886
HGNC1570
OMIM118444
RefSeqNM_000730
UniProtP32238
Other data
LocusChr. 4 p15.2-p15.1
cholecystokinin B receptor
Identifiers
SymbolCCKBR
NCBI gene887
HGNC1571
OMIM118445
RefSeqNM_176875
UniProtP32239
Other data
LocusChr. 11 p15.4

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) 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]

References

  1. "International Union of Pharmacology. XXI. Structure, distribution, and functions of cholecystokinin receptors". Pharmacological Reviews 51 (4): 745–781. December 1999. PMID 10581329. http://pharmrev.aspetjournals.org/cgi/pmidlookup?view=long&pmid=10581329. 
  2. "Cholecystokinin and gastrin receptors". Physiological Reviews 86 (3): 805–847. July 2006. doi:10.1152/physrev.00014.2005. PMID 16816139. 
  3. "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. doi:10.1152/ajpgi.1998.274.4.g607. PMID 9575840. 
  4. 4.0 4.1 "Cholecystokinin receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database" (in en). IUPHAR/BPS Guide to Pharmacology CITE 2019 (4). 2019-09-16. doi:10.2218/gtopdb/F15/2019.4. 

External links