Cholecystokinin B receptor: Difference between revisions

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{{Infobox_gene}}
{{PBB_Controls
The '''cholecystokinin B receptor''' also known as '''CCKBR''' or '''CCK<sub>2</sub>''' is a [[protein]]<ref name="pmid10368033">{{cite journal | vauthors = Noble F, Roques BP | title = CCK-B receptor: chemistry, molecular biology, biochemistry and pharmacology | journal = Progress in Neurobiology | volume = 58 | issue = 4 | pages = 349–79 | date = Jul 1999 | pmid = 10368033 | doi = 10.1016/S0301-0082(98)00090-2 }}</ref> that in humans is encoded by the ''CCKBR'' [[gene]].<ref name="pmid1280419">{{cite journal | vauthors = Pisegna JR, de Weerth A, Huppi K, Wank SA | title = Molecular cloning of the human brain and gastric cholecystokinin receptor: structure, functional expression and chromosomal localization | journal = Biochemical and Biophysical Research Communications | volume = 189 | issue = 1 | pages = 296–303 | date = Nov 1992 | pmid = 1280419 | doi = 10.1016/0006-291X(92)91557-7 }}</ref>
| update_page = yes
| require_manual_inspection = no
| update_protein_box = yes
| update_summary = yes
| update_citations = yes
}}


<!-- The GNF_Protein_box is automatically maintained by Protein Box Bot.  See Template:PBB_Controls to Stop updates. -->
This gene encodes a [[G protein-coupled receptor]] for [[gastrin]] and [[cholecystokinin]] (CCK),<ref name="pmid15520004">{{cite journal | vauthors = Harikumar KG, Clain J, Pinon DI, Dong M, Miller LJ | title = Distinct molecular mechanisms for agonist peptide binding to types A and B cholecystokinin receptors demonstrated using fluorescence spectroscopy | journal = The Journal of Biological Chemistry | volume = 280 | issue = 2 | pages = 1044–50 | date = Jan 2005 | pmid = 15520004 | doi = 10.1074/jbc.M409480200 }}</ref><ref name="pmid15001692">{{cite journal | vauthors = Aloj L, Caracò C, Panico M, Zannetti A, Del Vecchio S, Tesauro D, De Luca S, Arra C, Pedone C, Morelli G, Salvatore M | title = In vitro and in vivo evaluation of 111In-DTPAGlu-G-CCK8 for cholecystokinin-B receptor imaging | journal = Journal of Nuclear Medicine | volume = 45 | issue = 3 | pages = 485–94 | date = Mar 2004 | pmid = 15001692 | doi = }}</ref><ref name="pmid12695525">{{cite journal | vauthors = Galés C, Poirot M, Taillefer J, Maigret B, Martinez J, Moroder L, Escrieut C, Pradayrol L, Fourmy D, Silvente-Poirot S | title = 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 | journal = Molecular Pharmacology | volume = 63 | issue = 5 | pages = 973–82 | date = May 2003 | pmid = 12695525 | doi = 10.1124/mol.63.5.973 }}</ref> 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.<ref name="entrez">{{cite web | title = Entrez Gene: CCKBR cholecystokinin B receptor| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=887| accessdate = }}</ref>
{{GNF_Protein_box
| image = PBB_Protein_CCKBR_image.jpg
| image_source = [[Protein_Data_Bank|PDB]] rendering based on 1l4t.
| PDB = {{PDB2|1l4t}}
| Name = Cholecystokinin B receptor
| HGNCid = 1571
| Symbol = CCKBR
| AltSymbols =; CCK-B; GASR
| OMIM = 118445
| ECnumber =
| Homologene = 7258
| MGIid = 99479
| GeneAtlas_image1 = PBB_GE_CCKBR_210381_s_at_tn.png
| Function = {{GNF_GO|id=GO:0001584 |text = rhodopsin-like receptor activity}} {{GNF_GO|id=GO:0004435 |text = phosphoinositide phospholipase C activity}} {{GNF_GO|id=GO:0004872 |text = receptor activity}} {{GNF_GO|id=GO:0015054 |text = gastrin receptor activity}} {{GNF_GO|id=GO:0046935 |text = phosphatidylinositol 3-kinase regulator activity}}
| Component = {{GNF_GO|id=GO:0005886 |text = plasma membrane}} {{GNF_GO|id=GO:0005887 |text = integral to plasma membrane}}  
| Process = {{GNF_GO|id=GO:0007202 |text = phospholipase C activation}} {{GNF_GO|id=GO:0007204 |text = elevation of cytosolic calcium ion concentration}} {{GNF_GO|id=GO:0007586 |text = digestion}} {{GNF_GO|id=GO:0007600 |text = sensory perception}} {{GNF_GO|id=GO:0007631 |text = feeding behavior}} {{GNF_GO|id=GO:0008283 |text = cell proliferation}} {{GNF_GO|id=GO:0008284 |text = positive regulation of cell proliferation}}
| Orthologs = {{GNF_Ortholog_box
    | Hs_EntrezGene = 887
    | Hs_Ensembl = ENSG00000110148
    | Hs_RefseqProtein = NP_795344
    | Hs_RefseqmRNA = NM_176875
    | Hs_GenLoc_db =
    | Hs_GenLoc_chr = 11
    | Hs_GenLoc_start = 6237542
    | Hs_GenLoc_end = 6249932
    | Hs_Uniprot = P32239
    | Mm_EntrezGene = 12426
    | Mm_Ensembl = ENSMUSG00000030898
    | Mm_RefseqmRNA = NM_007627
    | Mm_RefseqProtein = NP_031653
    | Mm_GenLoc_db = 
    | Mm_GenLoc_chr = 7
    | Mm_GenLoc_start = 105299638
    | Mm_GenLoc_end = 105344719
    | Mm_Uniprot = Q3ZB46
  }}
}}
'''Cholecystokinin B receptor''', also known as '''CCKBR''', is a human [[gene]].


<!-- The PBB_Summary template is automatically maintained by Protein Box Bot. See Template:PBB_Controls to Stop updates. -->
== CNS effects ==
{{PBB_Summary
[[Cholecystokinin|CCK]] receptors significantly influence neurotransmission in the brain, regulating anxiety, feeding, and locomotion. CCK-B expression may correlate parallel to anxiety and depression phenotypes in humans. CCK-B receptors possess a complex regulation of [[dopamine]] activity in the brain. CCK-B activation appears to possess a general inhibitory action on dopamine activity in the brain, opposing the [[dopamine]]-enhancing effects of [[cholecystokinin A receptor|CCK-A]]. However, the effects of CCK-B on [[dopamine]] activity vary depending on location.<ref name="pmid2706523">{{cite journal | vauthors = Altar CA, Boyar WC | title = Brain CCK-B receptors mediate the suppression of dopamine release by cholecystokinin | journal = Brain Research | volume = 483 | issue = 2 | pages = 321–6 | date = Apr 1989 | pmid = 2706523 | doi = 10.1016/0006-8993(89)90176-5 }}</ref> CCK-B antagonism enhances dopamine release in rat striatum.<ref name="Loonam_2003">{{cite journal | vauthors = Loonam TM, Noailles PA, Yu J, Zhu JP, Angulo JA | title = Substance P and cholecystokinin regulate neurochemical responses to cocaine and methamphetamine in the striatum | journal = Life Sciences | volume = 73 | issue = 6 | pages = 727–39 | date = Jun 2003 | pmid = 12801594 | doi = 10.1016/S0024-3205(03)00393-X }}</ref> Activation enhances [[GABA]] release in rat anterior [[nucleus accumbens]].<ref name="pmid10651144">{{cite journal | vauthors = Lanza M, Makovec F | title = Cholecystokinin (CCK) increases GABA release in the rat anterior nucleus accumbens via CCK(B) receptors located on glutamatergic interneurons | journal = Naunyn-Schmiedeberg's Archives of Pharmacology | volume = 361 | issue = 1 | pages = 33–8 | date = Jan 2000 | pmid = 10651144 | doi = 10.1007/s002109900161 }}</ref> CCK-B receptors modulate dopamine release, and influence the development of tolerance to [[opioids]].<ref name="pmid2311658">{{cite journal | vauthors = Dourish CT, O'Neill MF, Coughlan J, Kitchener SJ, Hawley D, Iversen SD | title = The selective CCK-B receptor antagonist L-365,260 enhances morphine analgesia and prevents morphine tolerance in the rat | journal = European Journal of Pharmacology | volume = 176 | issue = 1 | pages = 35–44 | date = Jan 1990 | pmid = 2311658 | doi = 10.1016/0014-2999(90)90129-T }}</ref> CCK-B activation decreases amphetamine-induced DA release, and contributes to individual variability in response to amphetamine.<ref name="pmid7972279">{{cite journal | vauthors = Higgins GA, Sills TL, Tomkins DM, Sellers EM, Vaccarino FJ | title = Evidence for the contribution of CCKB receptor mechanisms to individual differences in amphetamine-induced locomotion | journal = Pharmacology Biochemistry and Behavior | volume = 48 | issue = 4 | pages = 1019–24 | date = Aug 1994 | pmid = 7972279 | doi = 10.1016/0091-3057(94)90214-3 }}</ref>
| section_title =  
| summary_text = 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.<ref name="entrez">{{cite web | title = Entrez Gene: CCKBR cholecystokinin B receptor| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=887| accessdate = }}</ref>
}}


==See also==
In rats, CCK-B antagonism prevents the stress-induced reactivation of [[cocaine]]-induced [[conditioned place preference]], and prevents the long-term maintenance and reinstatement of [[morphine]]-induced CPP.<ref name="pmid11173090">{{cite journal | vauthors = Lu L, Huang M, Ma L, Li J | title = Different role of cholecystokinin (CCK)-A and CCK-B receptors in relapse to morphine dependence in rats | journal = Behavioural Brain Research | volume = 120 | issue = 1 | pages = 105–10 | date = Apr 2001 | pmid = 11173090 | doi = 10.1016/S0166-4328(00)00361-2 }}</ref> Blockade of CCK-B potentiates cocaine-induced dopamine overflow in rat striatum.<ref name="Loonam_2003"/>  CCK-B may pose a modulatory role in parkinson's disease. Blockade of CCK-B in dopamine-depleted [[squirrel monkeys]] induces significant enhancement of [[Animal locomotion|locomotor]] response to [[L-DOPA]].<ref name="pmid1976438">{{cite journal | vauthors = Boyce S, Rupniak NM, Tye S, Steventon MJ, Iversen SD | title = Modulatory role for CCK-B antagonists in Parkinson's disease | journal = Clinical Neuropharmacology | volume = 13 | issue = 4 | pages = 339–47 | date = Aug 1990 | pmid = 1976438 | doi = 10.1097/00002826-199008000-00009 | url = http://journals.lww.com/clinicalneuropharm/Abstract/1990/08000/Modulatory_Role_for_CCK_B_Antagonists_in.9.aspx }}</ref> One study shows that visual hallucinations in Parkinson's disease are associated with cholecystokinin −45C>T polymorphism, and this association is still observed in the presence of the cholecystokinin-A receptor TC/CC genotype, indicating a possible interaction of these two genes in the visual hallucinogenesis in Parkinson's disease.<ref name="pmid12777967">{{cite journal | vauthors = Wang J, Si YM, Liu ZL, Yu L | title = Cholecystokinin, cholecystokinin-A receptor and cholecystokinin-B receptor gene polymorphisms in Parkinson's disease | journal = Pharmacogenetics | volume = 13 | issue = 6 | pages = 365–9 | date = Jun 2003 | pmid = 12777967 | doi = 10.1097/00008571-200306000-00008 }}</ref>
 
== Gastrointestinal Tract ==
The cholecystokinin B receptor is stimulated by CCK and gastrin in the stomach during digestion.
 
== Selective Ligands ==
The cholecystokinin B receptor responds to a number of ligands.
 
=== Agonists ===
* [[Cholecystokinin]]
* [[CCK-4]]
* [[Gastrin]]
* BBL-454
 
===Antagonists===
* [[Proglumide]]
* [[CI-988]]
* CI-1015
* L-365,260
* L-369,293
* YF476
* YM-022
* RP-69758
* LY-225,910
* LY-288,513
* PD-135,158
* PD-145,942
 
===Inverse agonists===
* L-740,093
 
== See also ==
* [[Cholecystokinin receptor]]
* [[Cholecystokinin receptor]]
* [[Cholecystokinin antagonist]]
* [[Cholecystokinin antagonist]]


==References==
== References ==
{{reflist|2}}
{{reflist|33em}}


==Further reading==
== Further reading ==
{{refbegin | 2}}
{{refbegin|33em}}
{{PBB_Further_reading
* {{cite journal | vauthors = Herget T, Sethi T, Wu SV, Walsh JH, Rozengurt E | title = Cholecystokinin stimulates Ca2+ mobilization and clonal growth in small cell lung cancer through CCKA and CCKB/gastrin receptors | journal = Annals of the New York Academy of Sciences | volume = 713 | issue =  | pages = 283–97 | date = Mar 1994 | pmid = 8185170 | doi = 10.1111/j.1749-6632.1994.tb44076.x }}
| citations =
* {{cite journal | vauthors = Lee YM, Beinborn M, McBride EW, Lu M, Kolakowski LF, Kopin AS | title = The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization | journal = The Journal of Biological Chemistry | volume = 268 | issue = 11 | pages = 8164–9 | date = Apr 1993 | pmid = 7681836 | doi =  }}
*{{cite journal | author=Herget T, Sethi T, Wu SV, ''et al.'' |title=Cholecystokinin stimulates Ca2+ mobilization and clonal growth in small cell lung cancer through CCKA and CCKB/gastrin receptors. |journal=Ann. N. Y. Acad. Sci. |volume=713 |issue=  |pages= 283-97 |year= 1994 |pmid= 8185170 |doi= }}
* {{cite journal | vauthors = Ito M, Iwata N, Taniguchi T, Murayama T, Chihara K, Matsui T | title = Functional characterization of two cholecystokinin-B/gastrin receptor isoforms: a preferential splice donor site in the human receptor gene | journal = Cell Growth & Differentiation | volume = 5 | issue = 10 | pages = 1127–35 | date = Oct 1994 | pmid = 7848914 | doi =  }}
*{{cite journal | author=Pisegna JR, de Weerth A, Huppi K, Wank SA |title=Molecular cloning of the human brain and gastric cholecystokinin receptor: structure, functional expression and chromosomal localization. |journal=Biochem. Biophys. Res. Commun. |volume=189 |issue= 1 |pages= 296-303 |year= 1992 |pmid= 1280419 |doi=  }}
* {{cite journal | vauthors = Miyake A | title = A truncated isoform of human CCK-B/gastrin receptor generated by alternative usage of a novel exon | journal = Biochemical and Biophysical Research Communications | volume = 208 | issue = 1 | pages = 230–7 | date = Mar 1995 | pmid = 7887934 | doi = 10.1006/bbrc.1995.1328 }}
*{{cite journal | author=Lee YM, Beinborn M, McBride EW, ''et al.'' |title=The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization. |journal=J. Biol. Chem. |volume=268 |issue= 11 |pages= 8164-9 |year= 1993 |pmid= 7681836 |doi=  }}
* {{cite journal | vauthors = Maruyama K, Sugano S | title = Oligo-capping: a simple method to replace the cap structure of eukaryotic mRNAs with oligoribonucleotides | journal = Gene | volume = 138 | issue = 1–2 | pages = 171–4 | date = Jan 1994 | pmid = 8125298 | doi = 10.1016/0378-1119(94)90802-8 }}
*{{cite journal | author=Ito M, Iwata N, Taniguchi T, ''et al.'' |title=Functional characterization of two cholecystokinin-B/gastrin receptor isoforms: a preferential splice donor site in the human receptor gene. |journal=Cell Growth Differ. |volume=5 |issue= 10 |pages= 1127-35 |year= 1995 |pmid= 7848914 |doi= }}
* {{cite journal | vauthors = Zimonjic DB, Popescu NC, Matsui T, Ito M, Chihara K | title = Localization of the human cholecystokinin-B/gastrin receptor gene (CCKBR) to chromosome 11p15.5-->p15.4 by fluorescence in situ hybridization | journal = Cytogenetics and Cell Genetics | volume = 65 | issue = 3 | pages = 184–5 | year = 1993 | pmid = 8222757 | doi = 10.1159/000133628 }}
*{{cite journal | author=Miyake A |title=A truncated isoform of human CCK-B/gastrin receptor generated by alternative usage of a novel exon. |journal=Biochem. Biophys. Res. Commun. |volume=208 |issue= 1 |pages= 230-7 |year= 1995 |pmid= 7887934 |doi= 10.1006/bbrc.1995.1328 }}
* {{cite journal | vauthors = de Weerth A, Pisegna JR, Huppi K, Wank SA | title = Molecular cloning, functional expression and chromosomal localization of the human cholecystokinin type A receptor | journal = Biochemical and Biophysical Research Communications | volume = 194 | issue = 2 | pages = 811–8 | date = Jul 1993 | pmid = 8343165 | doi = 10.1006/bbrc.1993.1894 }}
*{{cite journal | author=Maruyama K, Sugano S |title=Oligo-capping: a simple method to replace the cap structure of eukaryotic mRNAs with oligoribonucleotides. |journal=Gene |volume=138 |issue= 1-2 |pages= 171-4 |year= 1994 |pmid= 8125298 |doi= }}
* {{cite journal | vauthors = Ito M, Matsui T, Taniguchi T, Tsukamoto T, Murayama T, Arima N, Nakata H, Chiba T, Chihara K | title = Functional characterization of a human brain cholecystokinin-B receptor. A trophic effect of cholecystokinin and gastrin | journal = The Journal of Biological Chemistry | volume = 268 | issue = 24 | pages = 18300–5 | date = Aug 1993 | pmid = 8349705 | doi =  }}
*{{cite journal | author=Zimonjic DB, Popescu NC, Matsui T, ''et al.'' |title=Localization of the human cholecystokinin-B/gastrin receptor gene (CCKBR) to chromosome 11p15.5-->p15.4 by fluorescence in situ hybridization. |journal=Cytogenet. Cell Genet. |volume=65 |issue= 3 |pages= 184-5 |year= 1993 |pmid= 8222757 |doi= }}
* {{cite journal | vauthors = Song I, Brown DR, Wiltshire RN, Gantz I, Trent JM, Yamada T | title = The human gastrin/cholecystokinin type B receptor gene: alternative splice donor site in exon 4 generates two variant mRNAs | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 90 | issue = 19 | pages = 9085–9 | date = Oct 1993 | pmid = 8415658 | pmc = 47506 | doi = 10.1073/pnas.90.19.9085 }}
*{{cite journal | author=de Weerth A, Pisegna JR, Huppi K, Wank SA |title=Molecular cloning, functional expression and chromosomal localization of the human cholecystokinin type A receptor. |journal=Biochem. Biophys. Res. Commun. |volume=194 |issue= 2 |pages= 811-8 |year= 1993 |pmid= 8343165 |doi=  }}
* {{cite journal | vauthors = Beinborn M, Lee YM, McBride EW, Quinn SM, Kopin AS | title = A single amino acid of the cholecystokinin-B/gastrin receptor determines specificity for non-peptide antagonists | journal = Nature | volume = 362 | issue = 6418 | pages = 348–50 | date = Mar 1993 | pmid = 8455720 | doi = 10.1038/362348a0 }}
*{{cite journal | author=Ito M, Matsui T, Taniguchi T, ''et al.'' |title=Functional characterization of a human brain cholecystokinin-B receptor. A trophic effect of cholecystokinin and gastrin. |journal=J. Biol. Chem. |volume=268 |issue= 24 |pages= 18300-5 |year= 1993 |pmid= 8349705 |doi= }}
* {{cite journal | vauthors = Silvente-Poirot S, Wank SA | title = 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 | journal = The Journal of Biological Chemistry | volume = 271 | issue = 25 | pages = 14698–706 | date = Jun 1996 | pmid = 8663021 | doi = 10.1074/jbc.271.25.14698 }}
*{{cite journal | author=Song I, Brown DR, Wiltshire RN, ''et al.'' |title=The human gastrin/cholecystokinin type B receptor gene: alternative splice donor site in exon 4 generates two variant mRNAs. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=90 |issue= 19 |pages= 9085-9 |year= 1993 |pmid= 8415658 |doi= }}
* {{cite journal | vauthors = Tarasova NI, Wank SA, Hudson EA, Romanov VI, Czerwinski G, Resau JH, Michejda CJ | title = Endocytosis of gastrin in cancer cells expressing gastrin/CCK-B receptor | journal = Cell and Tissue Research | volume = 287 | issue = 2 | pages = 325–33 | date = Feb 1997 | pmid = 8995203 | doi = 10.1007/s004410050757 }}
*{{cite journal | author=Beinborn M, Lee YM, McBride EW, ''et al.'' |title=A single amino acid of the cholecystokinin-B/gastrin receptor determines specificity for non-peptide antagonists. |journal=Nature |volume=362 |issue= 6418 |pages= 348-50 |year= 1993 |pmid= 8455720 |doi= 10.1038/362348a0 }}
* {{cite journal | vauthors = Suzuki Y, Yoshitomo-Nakagawa K, Maruyama K, Suyama A, Sugano S | title = Construction and characterization of a full length-enriched and a 5'-end-enriched cDNA library | journal = Gene | volume = 200 | issue = 1–2 | pages = 149–56 | date = Oct 1997 | pmid = 9373149 | doi = 10.1016/S0378-1119(97)00411-3 }}
*{{cite journal | author=Silvente-Poirot S, Wank SA |title=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. |journal=J. Biol. Chem. |volume=271 |issue= 25 |pages= 14698-706 |year= 1996 |pmid= 8663021 |doi= }}
* {{cite journal | vauthors = O'Briant KC, Ali SY, Weier HU, Bepler G | title = 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 | journal = Chromosome Research | volume = 6 | issue = 5 | pages = 415–8 | date = Aug 1998 | pmid = 9872672 | doi = 10.1023/A:1009289625352 }}
*{{cite journal | author=Tarasova NI, Wank SA, Hudson EA, ''et al.'' |title=Endocytosis of gastrin in cancer cells expressing gastrin/CCK-B receptor. |journal=Cell Tissue Res. |volume=287 |issue= 2 |pages= 325-33 |year= 1997 |pmid= 8995203 |doi= }}
* {{cite journal | vauthors = Monstein HJ, Nilsson I, Ellnebo-Svedlund K, Svensson SP | title = Cloning and characterization of 5'-end alternatively spliced human cholecystokinin-B receptor mRNAs | journal = Receptors & Channels | volume = 6 | issue = 3 | pages = 165–77 | year = 1999 | pmid = 10100325 | doi =  }}
*{{cite journal | author=Suzuki Y, Yoshitomo-Nakagawa K, Maruyama K, ''et al.'' |title=Construction and characterization of a full length-enriched and a 5'-end-enriched cDNA library. |journal=Gene |volume=200 |issue= 1-2 |pages= 149-56 |year= 1997 |pmid= 9373149 |doi= }}
* {{cite journal | vauthors = Daulhac L, Kowalski-Chauvel A, Pradayrol L, Vaysse N, Seva C | title = Src-family tyrosine kinases in activation of ERK-1 and p85/p110-phosphatidylinositol 3-kinase by G/CCKB receptors | journal = The Journal of Biological Chemistry | volume = 274 | issue = 29 | pages = 20657–63 | date = Jul 1999 | pmid = 10400698 | doi = 10.1074/jbc.274.29.20657 }}
*{{cite journal | author=O'Briant KC, Ali SY, Weier HU, Bepler G |title=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. |journal=Chromosome Res. |volume=6 |issue= 5 |pages= 415-8 |year= 1999 |pmid= 9872672 |doi=  }}
* {{cite journal | vauthors = Silvente-Poirot S, Escrieut C, Galès C, Fehrentz JA, Escherich A, Wank SA, Martinez J, Moroder L, Maigret B, Bouisson M, Vaysse N, Fourmy D | title = 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 | journal = The Journal of Biological Chemistry | volume = 274 | issue = 33 | pages = 23191–7 | date = Aug 1999 | pmid = 10438490 | doi = 10.1074/jbc.274.33.23191 }}
*{{cite journal | author=Monstein HJ, Nilsson I, Ellnebo-Svedlund K, Svensson SP |title=Cloning and characterization of 5'-end alternatively spliced human cholecystokinin-B receptor mRNAs. |journal=Recept. Channels |volume=6 |issue= 3 |pages= 165-77 |year= 1999 |pmid= 10100325 |doi= }}
* {{cite journal | vauthors = Kulaksiz H, Arnold R, Göke B, Maronde E, Meyer M, Fahrenholz F, Forssmann WG, Eissele R | title = Expression and cell-specific localization of the cholecystokinin B/gastrin receptor in the human stomach | journal = Cell and Tissue Research | volume = 299 | issue = 2 | pages = 289–98 | date = Feb 2000 | pmid = 10741470 | doi = 10.1007/s004410050027 }}
*{{cite journal | author=Daulhac L, Kowalski-Chauvel A, Pradayrol L, ''et al.'' |title=Src-family tyrosine kinases in activation of ERK-1 and p85/p110-phosphatidylinositol 3-kinase by G/CCKB receptors. |journal=J. Biol. Chem. |volume=274 |issue= 29 |pages= 20657-63 |year= 1999 |pmid= 10400698 |doi= }}
*{{cite journal | author=Silvente-Poirot S, Escrieut C, Galès C, ''et al.'' |title=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. |journal=J. Biol. Chem. |volume=274 |issue= 33 |pages= 23191-7 |year= 1999 |pmid= 10438490 |doi= }}
*{{cite journal  | author=Kulaksiz H, Arnold R, Göke B, ''et al.'' |title=Expression and cell-specific localization of the cholecystokinin B/gastrin receptor in the human stomach. |journal=Cell Tissue Res. |volume=299 |issue= 2 |pages= 289-98 |year= 2000 |pmid= 10741470 |doi=  }}
}}
{{refend}}
{{refend}}


{{NLM content}}
{{NLM content}}
{{membrane-protein-stub}}
{{PDB Gallery|geneid=887}}
{{G protein-coupled receptors}}
{{G protein-coupled receptors}}
{{Neuropeptide receptors}}
{{Neuropeptide receptors}}
[[Category:G protein coupled receptors]]
{{Neuropeptidergics}}
 
[[Category:G protein-coupled receptors]]
[[Category:Cholecystokinin receptors]]

Latest revision as of 18:00, 24 September 2018

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Identifiers
Aliases
External IDsGeneCards: [1]
Orthologs
SpeciesHumanMouse
Entrez

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Ensembl

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UniProt

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RefSeq (mRNA)

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RefSeq (protein)

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Location (UCSC)n/an/a
PubMed searchn/an/a
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The cholecystokinin B receptor also known as CCKBR or CCK2 is a protein[1] that in humans is encoded by the CCKBR gene.[2]

This gene encodes a G protein-coupled receptor for gastrin and cholecystokinin (CCK),[3][4][5] 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.[6]

CNS effects

CCK receptors significantly influence neurotransmission in the brain, regulating anxiety, feeding, and locomotion. CCK-B expression may correlate parallel to anxiety and depression phenotypes in humans. CCK-B receptors possess a complex regulation of dopamine activity in the brain. CCK-B activation appears to possess a general inhibitory action on dopamine activity in the brain, opposing the dopamine-enhancing effects of CCK-A. However, the effects of CCK-B on dopamine activity vary depending on location.[7] CCK-B antagonism enhances dopamine release in rat striatum.[8] Activation enhances GABA release in rat anterior nucleus accumbens.[9] CCK-B receptors modulate dopamine release, and influence the development of tolerance to opioids.[10] CCK-B activation decreases amphetamine-induced DA release, and contributes to individual variability in response to amphetamine.[11]

In rats, CCK-B antagonism prevents the stress-induced reactivation of cocaine-induced conditioned place preference, and prevents the long-term maintenance and reinstatement of morphine-induced CPP.[12] Blockade of CCK-B potentiates cocaine-induced dopamine overflow in rat striatum.[8] CCK-B may pose a modulatory role in parkinson's disease. Blockade of CCK-B in dopamine-depleted squirrel monkeys induces significant enhancement of locomotor response to L-DOPA.[13] One study shows that visual hallucinations in Parkinson's disease are associated with cholecystokinin −45C>T polymorphism, and this association is still observed in the presence of the cholecystokinin-A receptor TC/CC genotype, indicating a possible interaction of these two genes in the visual hallucinogenesis in Parkinson's disease.[14]

Gastrointestinal Tract

The cholecystokinin B receptor is stimulated by CCK and gastrin in the stomach during digestion.

Selective Ligands

The cholecystokinin B receptor responds to a number of ligands.

Agonists

Antagonists

  • Proglumide
  • CI-988
  • CI-1015
  • L-365,260
  • L-369,293
  • YF476
  • YM-022
  • RP-69758
  • LY-225,910
  • LY-288,513
  • PD-135,158
  • PD-145,942

Inverse agonists

  • L-740,093

See also

References

  1. ↑ Noble F, Roques BP (Jul 1999). "CCK-B receptor: chemistry, molecular biology, biochemistry and pharmacology". Progress in Neurobiology. 58 (4): 349–79. doi:10.1016/S0301-0082(98)00090-2. PMID 10368033.
  2. ↑ Pisegna JR, de Weerth A, Huppi K, Wank SA (Nov 1992). "Molecular cloning of the human brain and gastric cholecystokinin receptor: structure, functional expression and chromosomal localization". Biochemical and Biophysical Research Communications. 189 (1): 296–303. doi:10.1016/0006-291X(92)91557-7. PMID 1280419.
  3. ↑ Harikumar KG, Clain J, Pinon DI, Dong M, Miller LJ (Jan 2005). "Distinct molecular mechanisms for agonist peptide binding to types A and B cholecystokinin receptors demonstrated using fluorescence spectroscopy". The Journal of Biological Chemistry. 280 (2): 1044–50. doi:10.1074/jbc.M409480200. PMID 15520004.
  4. ↑ Aloj L, Caracò C, Panico M, Zannetti A, Del Vecchio S, Tesauro D, De Luca S, Arra C, Pedone C, Morelli G, Salvatore M (Mar 2004). "In vitro and in vivo evaluation of 111In-DTPAGlu-G-CCK8 for cholecystokinin-B receptor imaging". Journal of Nuclear Medicine. 45 (3): 485–94. PMID 15001692.
  5. ↑ Galés C, Poirot M, Taillefer J, Maigret B, Martinez J, Moroder L, Escrieut C, Pradayrol L, Fourmy D, Silvente-Poirot S (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". Molecular Pharmacology. 63 (5): 973–82. doi:10.1124/mol.63.5.973. PMID 12695525.
  6. ↑ "Entrez Gene: CCKBR cholecystokinin B receptor".
  7. ↑ Altar CA, Boyar WC (Apr 1989). "Brain CCK-B receptors mediate the suppression of dopamine release by cholecystokinin". Brain Research. 483 (2): 321–6. doi:10.1016/0006-8993(89)90176-5. PMID 2706523.
  8. ↑ 8.0 8.1 Loonam TM, Noailles PA, Yu J, Zhu JP, Angulo JA (Jun 2003). "Substance P and cholecystokinin regulate neurochemical responses to cocaine and methamphetamine in the striatum". Life Sciences. 73 (6): 727–39. doi:10.1016/S0024-3205(03)00393-X. PMID 12801594.
  9. ↑ Lanza M, Makovec F (Jan 2000). "Cholecystokinin (CCK) increases GABA release in the rat anterior nucleus accumbens via CCK(B) receptors located on glutamatergic interneurons". Naunyn-Schmiedeberg's Archives of Pharmacology. 361 (1): 33–8. doi:10.1007/s002109900161. PMID 10651144.
  10. ↑ Dourish CT, O'Neill MF, Coughlan J, Kitchener SJ, Hawley D, Iversen SD (Jan 1990). "The selective CCK-B receptor antagonist L-365,260 enhances morphine analgesia and prevents morphine tolerance in the rat". European Journal of Pharmacology. 176 (1): 35–44. doi:10.1016/0014-2999(90)90129-T. PMID 2311658.
  11. ↑ Higgins GA, Sills TL, Tomkins DM, Sellers EM, Vaccarino FJ (Aug 1994). "Evidence for the contribution of CCKB receptor mechanisms to individual differences in amphetamine-induced locomotion". Pharmacology Biochemistry and Behavior. 48 (4): 1019–24. doi:10.1016/0091-3057(94)90214-3. PMID 7972279.
  12. ↑ Lu L, Huang M, Ma L, Li J (Apr 2001). "Different role of cholecystokinin (CCK)-A and CCK-B receptors in relapse to morphine dependence in rats". Behavioural Brain Research. 120 (1): 105–10. doi:10.1016/S0166-4328(00)00361-2. PMID 11173090.
  13. ↑ Boyce S, Rupniak NM, Tye S, Steventon MJ, Iversen SD (Aug 1990). "Modulatory role for CCK-B antagonists in Parkinson's disease". Clinical Neuropharmacology. 13 (4): 339–47. doi:10.1097/00002826-199008000-00009. PMID 1976438.
  14. ↑ Wang J, Si YM, Liu ZL, Yu L (Jun 2003). "Cholecystokinin, cholecystokinin-A receptor and cholecystokinin-B receptor gene polymorphisms in Parkinson's disease". Pharmacogenetics. 13 (6): 365–9. doi:10.1097/00008571-200306000-00008. PMID 12777967.

Further reading

  • Herget T, Sethi T, Wu SV, Walsh JH, Rozengurt E (Mar 1994). "Cholecystokinin stimulates Ca2+ mobilization and clonal growth in small cell lung cancer through CCKA and CCKB/gastrin receptors". Annals of the New York Academy of Sciences. 713: 283–97. doi:10.1111/j.1749-6632.1994.tb44076.x. PMID 8185170.
  • Lee YM, Beinborn M, McBride EW, Lu M, Kolakowski LF, Kopin AS (Apr 1993). "The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization". The Journal of Biological Chemistry. 268 (11): 8164–9. PMID 7681836.
  • Ito M, Iwata N, Taniguchi T, Murayama T, Chihara K, Matsui T (Oct 1994). "Functional characterization of two cholecystokinin-B/gastrin receptor isoforms: a preferential splice donor site in the human receptor gene". Cell Growth & Differentiation. 5 (10): 1127–35. PMID 7848914.
  • Miyake A (Mar 1995). "A truncated isoform of human CCK-B/gastrin receptor generated by alternative usage of a novel exon". Biochemical and Biophysical Research Communications. 208 (1): 230–7. doi:10.1006/bbrc.1995.1328. PMID 7887934.
  • Maruyama K, Sugano S (Jan 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, Ito M, Chihara K (1993). "Localization of the human cholecystokinin-B/gastrin receptor gene (CCKBR) to chromosome 11p15.5-->p15.4 by fluorescence in situ hybridization". Cytogenetics and Cell Genetics. 65 (3): 184–5. doi:10.1159/000133628. PMID 8222757.
  • de Weerth A, Pisegna JR, Huppi K, Wank SA (Jul 1993). "Molecular cloning, functional expression and chromosomal localization of the human cholecystokinin type A receptor". Biochemical and Biophysical Research Communications. 194 (2): 811–8. doi:10.1006/bbrc.1993.1894. PMID 8343165.
  • Ito M, Matsui T, Taniguchi T, Tsukamoto T, Murayama T, Arima N, Nakata H, Chiba T, Chihara K (Aug 1993). "Functional characterization of a human brain cholecystokinin-B receptor. A trophic effect of cholecystokinin and gastrin". The Journal of Biological Chemistry. 268 (24): 18300–5. PMID 8349705.
  • Song I, Brown DR, Wiltshire RN, Gantz I, Trent JM, Yamada T (Oct 1993). "The human gastrin/cholecystokinin type B receptor gene: alternative splice donor site in exon 4 generates two variant mRNAs". Proceedings of the National Academy of Sciences of the United States of America. 90 (19): 9085–9. doi:10.1073/pnas.90.19.9085. PMC 47506. PMID 8415658.
  • Beinborn M, Lee YM, McBride EW, Quinn SM, Kopin AS (Mar 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 (Jun 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". The Journal of Biological Chemistry. 271 (25): 14698–706. doi:10.1074/jbc.271.25.14698. PMID 8663021.
  • Tarasova NI, Wank SA, Hudson EA, Romanov VI, Czerwinski G, Resau JH, Michejda CJ (Feb 1997). "Endocytosis of gastrin in cancer cells expressing gastrin/CCK-B receptor". Cell and Tissue Research. 287 (2): 325–33. doi:10.1007/s004410050757. PMID 8995203.
  • Suzuki Y, Yoshitomo-Nakagawa K, Maruyama K, Suyama A, Sugano S (Oct 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 (Aug 1998). "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 Research. 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". Receptors & Channels. 6 (3): 165–77. PMID 10100325.
  • Daulhac L, Kowalski-Chauvel A, Pradayrol L, Vaysse N, Seva C (Jul 1999). "Src-family tyrosine kinases in activation of ERK-1 and p85/p110-phosphatidylinositol 3-kinase by G/CCKB receptors". The Journal of Biological Chemistry. 274 (29): 20657–63. doi:10.1074/jbc.274.29.20657. PMID 10400698.
  • Silvente-Poirot S, Escrieut C, Galès C, Fehrentz JA, Escherich A, Wank SA, Martinez J, Moroder L, Maigret B, Bouisson M, Vaysse N, Fourmy D (Aug 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". The Journal of Biological Chemistry. 274 (33): 23191–7. doi:10.1074/jbc.274.33.23191. PMID 10438490.
  • Kulaksiz H, Arnold R, Göke B, Maronde E, Meyer M, Fahrenholz F, Forssmann WG, Eissele R (Feb 2000). "Expression and cell-specific localization of the cholecystokinin B/gastrin receptor in the human stomach". Cell and Tissue Research. 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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