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cholecystokinin A receptor
Identifiers
SymbolCCKAR
NCBI gene 886
HGNC 1570
OMIM 118444
RefSeq NM_000730
UniProt P32238
Other data
Locus Chr. 4 p15.2-p15.1
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Structures Swiss-model
Domains InterPro
cholecystokinin B receptor
Identifiers
SymbolCCKBR
NCBI gene 887
HGNC 1571
OMIM 118445
RefSeq NM_176875
UniProt P32239
Other data
Locus Chr. 11 p15.4
Search for
Structures Swiss-model
Domains InterPro

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. ^ 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. ^ a b 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.

External links