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Gene Review

CCKAR  -  cholecystokinin A receptor

Homo sapiens

Synonyms: CCK-A, CCK-A receptor, CCK-AR, CCK1-R, CCK1R, ...
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Disease relevance of CCKAR


Psychiatry related information on CCKAR


High impact information on CCKAR


Chemical compound and disease context of CCKAR


Biological context of CCKAR

  • CONCLUSIONS: The data from the case control suggest that polymorphisms of the promoter region of the CCKAR gene do not play a major role in the pathogenesis of alcohol withdrawal symptoms or alcoholic liver injury [5].
  • The human CCKAR gene maps to chromosome 4 [15].
  • Investigation of quantitative trait loci in the CCKAR gene with susceptibility to alcoholism [5].
  • In addition, patients displaying hallucinations showed a higher frequency of the homozygous genotype of the allele (GT)8 at the -388 locus of the CCKAR gene (p = .042) and homo- and heterozygous genotypes of the T allele at the -333 locus (p = .025), relative to other patients [16].
  • These first molecular data identifying the agonist binding site of the human CCK-A receptor represent an important step toward the complete delineation of the agonist binding site and the understanding of the molecular mechanisms that govern differential activation of this receptor by CCK-related peptides [17].

Anatomical context of CCKAR


Associations of CCKAR with chemical compounds

  • First intracellular loop of the human cholecystokinin-A receptor is essential for cyclic AMP signaling in transfected HEK-293 cells [22].
  • Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent [23].
  • Analogs of the previously reported 1,5-benzodiazepine peripheral cholecystokinin (CCK-A) receptor agonist 1 were prepared which explore substitution and/or replacement of the C-3 phenyl urea moiety [23].
  • The potency of the contraction induced by CCK-8, desulphated CCK-8, and gastrin-I, and the effect of the CCK-A (loxiglumide and SR 27897) and the CCK-B (YM022 and L-365 260) specific receptor antagonists were compared [24].
  • In contrast, its enantiomer PD 140548 ((benzenebutanoic acid, beta-[[3-(1H-indol-3-yl)-2-methyl-1-oxo-2-[[(tricyclo[,7] dec-2-yloxy)carbonyl]amino]propyl] amino],-[S-(R*,S*)) displayed the reverse selectivity (CCKA IC50 = 2.8 nM, CCKB IC50 = 260 nM) [25].

Physical interactions of CCKAR


Regulatory relationships of CCKAR

  • This segment could account for 100 of the expected 300-fold lower affinity of gastrin-17-I observed for the control CCKAR compared to the control CCKBR [26].
  • Furthermore, the selective CCKA antagonist CAM-1481 inhibited the increase in [Ca2+]i induced by CCK-8 (half-maximal inhibitory concentration = 3 nM) in GLC19 but not in H510 cells [27].
  • Gastrin stimulates growth of human colon cancer cells via a receptor other than CCK-A or CCK-B [28].
  • CCK-B antagonists suppressed CCK-4-induced calcium mobilization more potently than CCK-A antagonist [29].
  • The present work shows that both aminosteroids inhibit cholecystokinin-(26-33)-peptide amide (CCK-8)-induced phospholipase D activation equipotently in Chinese hamster ovary cells expressing the cholecystokinin-A receptor (CHO-CCK(A) cells) [30].

Other interactions of CCKAR


Analytical, diagnostic and therapeutic context of CCKAR


  1. Regulation of growth of human gastric cancer by gastrin and glycine-extended progastrin. Iwase, K., Evers, B.M., Hellmich, M.R., Guo, Y.S., Higashide, S., Kim, H.J., Townsend, C.M. Gastroenterology (1997) [Pubmed]
  2. Genetic, pharmacological and functional analysis of cholecystokinin-1 and cholecystokinin-2 receptor polymorphism in type 2 diabetes and obese patients. Marchal-Victorion, S., Vionnet, N., Escrieut, C., Dematos, F., Dina, C., Dufresne, M., Vaysse, N., Pradayrol, L., Froguel, P., Fourmy, D. Pharmacogenetics (2002) [Pubmed]
  3. Differential expression of the CCK-A and CCK-B/gastrin receptor genes in human cancers of the esophagus, stomach and colon. Clerc, P., Dufresne, M., Saillan, C., Chastre, E., André, T., Escrieut, C., Kennedy, K., Vaysse, N., Gespach, C., Fourmy, D. Int. J. Cancer (1997) [Pubmed]
  4. Cholecystokinin, cholecystokinin-A receptor and cholecystokinin-B receptor gene polymorphisms in Parkinson's disease. Wang, J., Si, Y.M., Liu, Z.L., Yu, L. Pharmacogenetics (2003) [Pubmed]
  5. Investigation of quantitative trait loci in the CCKAR gene with susceptibility to alcoholism. Okubo, T., Harada, S., Higuchi, S., Matsushita, S. Alcohol. Clin. Exp. Res. (2002) [Pubmed]
  6. Association of cholecystokinin-A receptor gene polymorphisms and panic disorder in Japanese. Miyasaka, K., Yoshida, Y., Matsushita, S., Higuchi, S., Shirakawa, O., Shimokata, H., Funakoshi, A. Am. J. Med. Genet. B Neuropsychiatr. Genet. (2004) [Pubmed]
  7. Role of circulating cholecystokinin in control of fat-induced inhibition of food intake in humans. Drewe, J., Gadient, A., Rovati, L.C., Beglinger, C. Gastroenterology (1992) [Pubmed]
  8. Postponement of satiety by blockade of brain cholecystokinin (CCK-B) receptors. Dourish, C.T., Rycroft, W., Iversen, S.D. Science (1989) [Pubmed]
  9. Cholecystokinin A and B receptors are differentially expressed in normal pancreas and pancreatic adenocarcinoma. Weinberg, D.S., Ruggeri, B., Barber, M.T., Biswas, S., Miknyocki, S., Waldman, S.A. J. Clin. Invest. (1997) [Pubmed]
  10. The role of fat and cholecystokinin in functional dyspepsia. Fried, M., Feinle, C. Gut (2002) [Pubmed]
  11. Selective CCK-A but not CCK-B receptor antagonists inhibit HT-29 cell proliferation: synergism with pharmacological levels of melatonin. González-Puga, C., García-Navarro, A., Escames, G., León, J., López-Cantarero, M., Ros, E., Acuña-Castroviejo, D. J. Pineal Res. (2005) [Pubmed]
  12. CCK-JMV-180 acts as an antagonist of the CCKA receptor in the human IMR-32 neuroblastoma cell line. Schaeffer, P., Prabonnaud, V., Roux, M., Gully, D., Herbert, J.M. FEBS Lett. (1994) [Pubmed]
  13. His381 of the rat CCKB receptor is essential for CCKB versus CCKA receptor antagonist selectivity. Jagerschmidt, A., Guillaume-Rousselet, N., Vikland, M.L., Goudreau, N., Maigret, B., Roques, B.P. Eur. J. Pharmacol. (1996) [Pubmed]
  14. Vagal CCK and 5-HT(3) receptors are unlikely to mediate LPS or IL-1beta-induced fever. Martin, S.M., Wilson, B.C., Chen, X., Takahashi, Y., Poulin, P., Pittman, Q.J. Am. J. Physiol. Regul. Integr. Comp. Physiol. (2000) [Pubmed]
  15. Molecular cloning, functional expression and chromosomal localization of the human cholecystokinin type A receptor. de Weerth, A., Pisegna, J.R., Huppi, K., Wank, S.A. Biochem. Biophys. Res. Commun. (1993) [Pubmed]
  16. Polymorphisms of the CCK, CCKAR and CCKBR genes: an association with alcoholism study. Okubo, T., Harada, S. J. Stud. Alcohol (2001) [Pubmed]
  17. Identification of two amino acids of the human cholecystokinin-A receptor that interact with the N-terminal moiety of cholecystokinin. Kennedy, K., Gigoux, V., Escrieut, C., Maigret, B., Martinez, J., Moroder, L., Fréhel, D., Gully, D., Vaysse, N., Fourmy, D. J. Biol. Chem. (1997) [Pubmed]
  18. Cholecystokinin receptors in human pancreas and gallbladder muscle: a comparative study. Tang, C., Biemond, I., Lamers, C.B. Gastroenterology (1996) [Pubmed]
  19. Determination of RNA expression for cholecystokinin/gastrin receptors (CCKA, CCKB and CCKC) in human tumors of the central and peripheral nervous system. Lefranc, F., Chaboteaux, C., Belot, N., Brotchi, J., Salmon, I., Kiss, R. Int. J. Oncol. (2003) [Pubmed]
  20. Cholecystokinin A and B receptor mRNA expression in human pancreas. Nishimori, I., Kamakura, M., Fujikawa-Adachi, K., Nojima, M., Onishi, S., Hollingsworth, M.A., Harris, A. Pancreas (1999) [Pubmed]
  21. Mechanism of cholecystokinin-A- receptor antagonist on human pancreatic exocrine secretion. Localization of CCK-A receptor in the human duodenum. Funakoshi, A., Fukamizu, Y., Miyasaka, K. Digestion (1999) [Pubmed]
  22. First intracellular loop of the human cholecystokinin-A receptor is essential for cyclic AMP signaling in transfected HEK-293 cells. Wu, V., Yang, M., McRoberts, J.A., Ren, J., Seensalu, R., Zeng, N., Dagrag, M., Birnbaumer, M., Walsh, J.H. J. Biol. Chem. (1997) [Pubmed]
  23. Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent. Hirst, G.C., Aquino, C., Birkemo, L., Croom, D.K., Dezube, M., Dougherty, R.W., Ervin, G.N., Grizzle, M.K., Henke, B., James, M.K., Johnson, M.F., Momtahen, T., Queen, K.L., Sherrill, R.G., Szewczyk, J., Willson, T.M., Sugg, E.E. J. Med. Chem. (1996) [Pubmed]
  24. Pharmacological and molecular characterization of muscular cholecystokinin receptors in the human lower oesophageal sphincter. González, A.A., Farré, R., Monés, J., Capellà, G., Clavé, P. Neurogastroenterol. Motil. (2000) [Pubmed]
  25. Peptoid CCK receptor antagonists: pharmacological evaluation of CCKA, CCKB and mixed CCKA/B receptor antagonists. Singh, L., Field, M.J., Hill, D.R., Horwell, D.C., McKnight, A.T., Roberts, E., Tang, K.W., Woodruff, G.N. Eur. J. Pharmacol. (1995) [Pubmed]
  26. A segment of five amino acids in the second extracellular loop of the cholecystokinin-B receptor is essential for selectivity of the peptide agonist gastrin. Silvente-Poirot, S., Wank, S.A. J. Biol. Chem. (1996) [Pubmed]
  27. CCKA and CCKB receptors are expressed in small cell lung cancer lines and mediate Ca2+ mobilization and clonal growth. Sethi, T., Herget, T., Wu, S.V., Walsh, J.H., Rozengurt, E. Cancer Res. (1993) [Pubmed]
  28. Gastrin stimulates growth of human colon cancer cells via a receptor other than CCK-A or CCK-B. Bold, R.J., Ishizuka, J., Townsend, C.M., Thompson, J.C. Biochem. Biophys. Res. Commun. (1994) [Pubmed]
  29. CCK-4-induced calcium mobilization in T cells is enhanced in panic disorder. Akiyoshi, J., Moriyama, T., Isogawa, K., Miyamoto, M., Sasaki, I., Kuga, K., Yamamoto, H., Yamada, K., Fujii, I. J. Neurochem. (1996) [Pubmed]
  30. U73122 and U73343 inhibit receptor-mediated phospholipase D activation downstream of phospholipase C in CHO cells. Bosch, R.R., Patel, A.M., Van Emst-de Vries, S.E., Smeets, R.L., De Pont, J.J., Willems, P.H. Eur. J. Pharmacol. (1998) [Pubmed]
  31. Physiological role of cholecystokinin in gastroprotection in humans. Konturek, J.W., Hengst, K., Konturek, S.J., Sito, E., Stachura, J., Domschke, W. Am. J. Gastroenterol. (1998) [Pubmed]
  32. The effect of bombesin, cholecystokinin, gastrin, and their antagonists on proliferation of pancreatic cancer cell lines. Ohlsson, B., Fredäng, N., Axelson, J. Scand. J. Gastroenterol. (1999) [Pubmed]
  33. Modeled structure of a G-protein-coupled receptor: the cholecystokinin-1 receptor. Archer-Lahlou, E., Tikhonova, I., Escrieut, C., Dufresne, M., Seva, C., Pradayrol, L., Moroder, L., Maigret, B., Fourmy, D. J. Med. Chem. (2005) [Pubmed]
  34. Human cholecystokinin type A receptor gene: cytogenetic localization, physical mapping, and identification of two missense variants in patients with obesity and non-insulin-dependent diabetes mellitus (NIDDM). Inoue, H., Iannotti, C.A., Welling, C.M., Veile, R., Donis-Keller, H., Permutt, M.A. Genomics (1997) [Pubmed]
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