Cholecystokinin B receptor: Wikis


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Cholecystokinin B receptor

PDB rendering based on 1l4t.
Available structures
External IDs OMIM118445 MGI99479 HomoloGene7258 IUPHAR: CCK2 GeneCards: CCKBR Gene
RNA expression pattern
PBB GE CCKBR 210381 s at tn.png
More reference expression data
Species Human Mouse
Entrez 887 12426
Ensembl ENSG00000110148 ENSMUSG00000030898
UniProt P32239 Q3ZB46
RefSeq (mRNA) NM_176875 NM_007627
RefSeq (protein) NP_795344 NP_031653
Location (UCSC) Chr 11:
6.24 - 6.25 Mb
Chr 7:
105.3 - 105.34 Mb
PubMed search [1] [2]

The Cholecystokinin B receptor is a human protein that is also known as CCKBR or CCK2, with CCK2 now being the IUPHAR-recommended name.

This gene encodes a G-protein coupled receptor for gastrin and cholecystokinin (CCK), regulatory peptides of the brain and gastrointestinal tract. This protein is a type B gastrin receptor, which has a high affinity for both sulfated and nonsulfated CCK analogs and is found principally in the central nervous system and the gastrointestinal tract. A misspliced transcript variant including an intron has been observed in cells from colorectal and pancreatic tumors.[1]


Selective Ligands




  • Proglumide
  • CI-988
  • CI-1015
  • L-365,260
  • L-369,293
  • YF-476
  • YM-022
  • RP-69758
  • LY-225,910
  • LY-288,513
  • PD-135,158
  • PD-145,942

Inverse agonists

  • L-740,093


Cholecystokinin B receptor has been shown to interact with Cholecystokinin.[2][3][4]

See also


  1. ^ "Entrez Gene: CCKBR cholecystokinin B receptor".  
  2. ^ Harikumar, Kaleeckal G; Clain Jeremy, Pinon Delia I, Dong Maoqing, Miller Laurence J (Jan. 2005). "Distinct molecular mechanisms for agonist peptide binding to types A and B cholecystokinin receptors demonstrated using fluorescence spectroscopy". J. Biol. Chem. (United States) 280 (2): 1044–50. doi:10.1074/jbc.M409480200. ISSN 0021-9258. PMID 15520004.  
  3. ^ Aloj, Luigi; Caracò Corradina, Panico Mariarosaria, Zannetti Antonella, Del Vecchio Silvana, Tesauro Diego, De Luca Stefania, Arra Claudio, Pedone Carlo, Morelli Giancarlo, Salvatore Marco (Mar. 2004). "In vitro and in vivo evaluation of 111In-DTPAGlu-G-CCK8 for cholecystokinin-B receptor imaging". J. Nucl. Med. (United States) 45 (3): 485–94. ISSN 0161-5505. PMID 15001692.  
  4. ^ Galés, Céline; Poirot Marc, Taillefer Julien, Maigret Bernard, Martinez Jean, Moroder Luis, Escrieut Chantal, Pradayrol Lucien, Fourmy Daniel, Silvente-Poirot Sandrine (May. 2003). "Identification of tyrosine 189 and asparagine 358 of the cholecystokinin 2 receptor in direct interaction with the crucial C-terminal amide of cholecystokinin by molecular modeling, site-directed mutagenesis, and structure/affinity studies". Mol. Pharmacol. (United States) 63 (5): 973–82. ISSN 0026-895X. PMID 12695525.  

External links

Further reading

  • Herget T, Sethi T, Wu SV, et al. (1994). "Cholecystokinin stimulates Ca2+ mobilization and clonal growth in small cell lung cancer through CCKA and CCKB/gastrin receptors.". Ann. N. Y. Acad. Sci. 713: 283–97. doi:10.1111/j.1749-6632.1994.tb44076.x. PMID 8185170.  
  • Pisegna JR, de Weerth A, Huppi K, Wank SA (1992). "Molecular cloning of the human brain and gastric cholecystokinin receptor: structure, functional expression and chromosomal localization.". Biochem. Biophys. Res. Commun. 189 (1): 296–303. doi:10.1016/0006-291X(92)91557-7. PMID 1280419.  
  • Lee YM, Beinborn M, McBride EW, et al. (1993). "The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization.". J. Biol. Chem. 268 (11): 8164–9. PMID 7681836.  
  • Ito M, Iwata N, Taniguchi T, et al. (1995). "Functional characterization of two cholecystokinin-B/gastrin receptor isoforms: a preferential splice donor site in the human receptor gene.". Cell Growth Differ. 5 (10): 1127–35. PMID 7848914.  
  • Miyake A (1995). "A truncated isoform of human CCK-B/gastrin receptor generated by alternative usage of a novel exon.". Biochem. Biophys. Res. Commun. 208 (1): 230–7. doi:10.1006/bbrc.1995.1328. PMID 7887934.  
  • Maruyama K, Sugano S (1994). "Oligo-capping: a simple method to replace the cap structure of eukaryotic mRNAs with oligoribonucleotides.". Gene 138 (1-2): 171–4. doi:10.1016/0378-1119(94)90802-8. PMID 8125298.  
  • Zimonjic DB, Popescu NC, Matsui T, et al. (1993). "Localization of the human cholecystokinin-B/gastrin receptor gene (CCKBR) to chromosome 11p15.5→p15.4 by fluorescence in situ hybridization.". Cytogenet. Cell Genet. 65 (3): 184–5. doi:10.1159/000133628. PMID 8222757.  
  • de Weerth A, Pisegna JR, Huppi K, Wank SA (1993). "Molecular cloning, functional expression and chromosomal localization of the human cholecystokinin type A receptor.". Biochem. Biophys. Res. Commun. 194 (2): 811–8. doi:10.1006/bbrc.1993.1894. PMID 8343165.  
  • Ito M, Matsui T, Taniguchi T, et al. (1993). "Functional characterization of a human brain cholecystokinin-B receptor. A trophic effect of cholecystokinin and gastrin.". J. Biol. Chem. 268 (24): 18300–5. PMID 8349705.  
  • Song I, Brown DR, Wiltshire RN, et al. (1993). "The human gastrin/cholecystokinin type B receptor gene: alternative splice donor site in exon 4 generates two variant mRNAs.". Proc. Natl. Acad. Sci. U.S.A. 90 (19): 9085–9. doi:10.1073/pnas.90.19.9085. PMID 8415658.  
  • Beinborn M, Lee YM, McBride EW, et al. (1993). "A single amino acid of the cholecystokinin-B/gastrin receptor determines specificity for non-peptide antagonists.". Nature 362 (6418): 348–50. doi:10.1038/362348a0. PMID 8455720.  
  • Silvente-Poirot S, Wank SA (1996). "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.". J. Biol. Chem. 271 (25): 14698–706. doi:10.1074/jbc.271.25.14698. PMID 8663021.  
  • Tarasova NI, Wank SA, Hudson EA, et al. (1997). "Endocytosis of gastrin in cancer cells expressing gastrin/CCK-B receptor.". Cell Tissue Res. 287 (2): 325–33. doi:10.1007/s004410050757. PMID 8995203.  
  • Suzuki Y, Yoshitomo-Nakagawa K, Maruyama K, et al. (1997). "Construction and characterization of a full length-enriched and a 5'-end-enriched cDNA library.". Gene 200 (1-2): 149–56. doi:10.1016/S0378-1119(97)00411-3. PMID 9373149.  
  • O'Briant KC, Ali SY, Weier HU, Bepler G (1999). "An 84-kilobase physical map and repeat polymorphisms of the gastrin/cholecystokinin brain receptor region at the junction of chromosome segments 11p15.4 and 15.5.". Chromosome Res. 6 (5): 415–8. doi:10.1023/A:1009289625352. PMID 9872672.  
  • Monstein HJ, Nilsson I, Ellnebo-Svedlund K, Svensson SP (1999). "Cloning and characterization of 5'-end alternatively spliced human cholecystokinin-B receptor mRNAs.". Recept. Channels 6 (3): 165–77. PMID 10100325.  
  • Daulhac L, Kowalski-Chauvel A, Pradayrol L, et al. (1999). "Src-family tyrosine kinases in activation of ERK-1 and p85/p110-phosphatidylinositol 3-kinase by G/CCKB receptors.". J. Biol. Chem. 274 (29): 20657–63. doi:10.1074/jbc.274.29.20657. PMID 10400698.  
  • Silvente-Poirot S, Escrieut C, Galès C, et al. (1999). "Evidence for a direct interaction between the penultimate aspartic acid of cholecystokinin and histidine 207, located in the second extracellular loop of the cholecystokinin B receptor.". J. Biol. Chem. 274 (33): 23191–7. doi:10.1074/jbc.274.33.23191. PMID 10438490.  
  • Kulaksiz H, Arnold R, Göke B, et al. (2000). "Expression and cell-specific localization of the cholecystokinin B/gastrin receptor in the human stomach.". Cell Tissue Res. 299 (2): 289–98. doi:10.1007/s004410050027. PMID 10741470.  

This article incorporates text from the United States National Library of Medicine, which is in the public domain.


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