Cholecystokinin receptor
From Wikipedia, the free encyclopedia
Cholecystokinin receptors or CCK receptors are a group of G-protein coupled receptors which bind the peptide hormones cholecystokinin (CCK) or 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 |
| 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 |
| CCKB (CCK2) |
CCKBR |
primarily CNS, lesser amounts in the gastrointestinal tract |
gastrin ≈ CCK (receptor does not descriminate between sulfated and nonsulfated peptides) |
regulation of nociception, anxiety, memory and hunger |
[edit] References
- ^ 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): 745–81. PMID 10581329. http://pharmrev.aspetjournals.org/cgi/pmidlookup?view=long&pmid=10581329.
- ^ Dufresne M, Seva C, Fourmy D (2006). "Cholecystokinin and gastrin receptors". Physiol. Rev. 86 (3): 805–47. doi:10.1152/physrev.00014.2005. PMID 16816139.
[edit] External links
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Class A:
Rhodopsin like |
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Metabolites and
signaling molecules
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Peptide
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Miscellaneous
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| Class B: Secretin like |
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Class C: Metabotropic
glutamate / pheromone |
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Class F:
Frizzled / Smoothened |
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B trdu: iter (nrpl/grfl/cytl/horl), csrc (lgic, enzr, gprc, igsr, intg, nrpr/grfr/cytr), itra (adap, gbpr, mapk), calc, lipd; path (hedp, wntp, tgfp+mapp, notp, jakp, fsap, hipp, tlrp)
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| G protein-coupled receptor |
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Other neuropeptide receptors
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| Type I cytokine receptor |
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| Enzyme-linked receptor |
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| Other |
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B trdu: iter (nrpl/grfl/cytl/horl), csrc (lgic, enzr, gprc, igsr, intg, nrpr/grfr/cytr), itra (adap, gbpr, mapk), calc, lipd; path (hedp, wntp, tgfp+mapp, notp, jakp, fsap, hipp, tlrp)
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| Cholecystokinin |
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| CRH |
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| Galanin |
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| Ghrelin |
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| MCH |
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| Melanocortin |
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| Neuropeptide S |
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| Neuropeptide Y |
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| Neurotensin |
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| Opioid |
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| Orexin |
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| Oxytocin |
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| Tachykinin |
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- Agonists: Substance P
Antagonists: Aprepitant
- Befetupitant
- Casopitant
- CI-1021
- CP-96,345
- CP-99,994
- CP-122,721
- Dapitant
- Ezlopitant
- FK-888
- Fosaprepitant
- GR-203,040
- GW-597,599
- HSP-117
- L-733,060
- L-741,671
- L-743,310
- L-758,298
- Lanepitant
- LY-306,740
- Maropitant
- Netupitant
- NKP-608
- Nolpitantium
- Orvepitant
- RP-67,580
- SDZ NKT 343
- Vestipitant
- Vofopitant
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| Vasopressin |
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