- 関
- CCK-B receptor
WordNet
- the 2nd letter of the Roman alphabet (同)b
- the blood group whose red cells carry the B antigen (同)type_B, group B
- a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
- a gastrointestinal hormone that stimulates the secretion of pancreatic enzymes and the contraction and emptying of the gall bladder; its release is stimulated by the presence of fatty acids and amino acids in the small intestine
PrepTutorEJDIC
- =sense organ / 受信装置
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/03/21 22:41:38」(JST)
[Wiki en表示]
| Cholecystokinin B receptor |
NMR structure of the third extracellular loop of the human CCK-B receptor. PDB rendering based on 1l4t. |
| Available structures |
| PDB |
Ortholog search: PDBe, RCSB |
| List of PDB id codes |
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1L4T
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| Identifiers |
| Symbols |
CCKBR; CCK-B; CCK2R; GASR |
| External IDs |
OMIM: 118445 MGI: 99479 HomoloGene: 7258 IUPHAR: CCK2 ChEMBL: 298 GeneCards: CCKBR Gene |
| Gene Ontology |
| Molecular function |
• phosphatidylinositol phospholipase C activity
• cholecystokinin receptor activity
• gastrin receptor activity
• type B gastrin/cholecystokinin receptor binding
• 1-phosphatidylinositol-3-kinase regulator activity
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| Cellular component |
• nucleus
• cytoplasm
• plasma membrane
• integral to plasma membrane
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| Biological process |
• histamine secretion
• behavioral defense response
• apoptotic process
• cell surface receptor signaling pathway
• phospholipase C-activating G-protein coupled receptor signaling pathway
• elevation of cytosolic calcium ion concentration
• digestion
• sensory perception
• feeding behavior
• cell proliferation
• positive regulation of cell proliferation
• positive regulation of synaptic transmission, GABAergic
• response to insulin stimulus
• regulation of sensory perception of pain
• positive regulation of synaptic transmission, glutamatergic
• estrous cycle phase
• ERK1 and ERK2 cascade
• positive regulation of somatostatin secretion
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| Sources: Amigo / QuickGO |
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| RNA expression pattern |
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| More reference expression data |
| Orthologs |
| Species |
Human |
Mouse |
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| Entrez |
887 |
12426 |
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| Ensembl |
ENSG00000110148 |
ENSMUSG00000030898 |
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| UniProt |
P32239 |
P56481 |
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| RefSeq (mRNA) |
NM_176875 |
NM_007627 |
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| RefSeq (protein) |
NP_795344 |
NP_031653 |
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| Location (UCSC) |
Chr 11:
6.28 – 6.29 Mb |
Chr 7:
105.43 – 105.47 Mb |
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| PubMed search |
[1] |
[2] |
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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]
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Contents
- 1 CNS effects
- 2 Gastrointestinal Tract
- 3 Selective Ligands
- 3.1 Agonists
- 3.2 Antagonists
- 3.3 Inverse agonists
- 4 See also
- 5 References
- 6 Further reading
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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]
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
- YF-476
- YM-022
- RP-69758
- LY-225,910
- LY-288,513
- PD-135,158
- PD-145,942
Inverse agonists
See also
- Cholecystokinin receptor
- Cholecystokinin antagonist
References
- ^ Noble F, Roques BP (July 1999). "CCK-B receptor: chemistry, molecular biology, biochemistry and pharmacology". Prog. Neurobiol. 58 (4): 349–79. doi:10.1016/S0301-0082(98)00090-2. PMID 10368033.
- ^ Pisegna JR, de Weerth A, Huppi K, Wank SA (November 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.
- ^ Harikumar KG, Clain J, Pinon DI, Dong M, Miller LJ (January 2005). "Distinct molecular mechanisms for agonist peptide binding to types A and B cholecystokinin receptors demonstrated using fluorescence spectroscopy". J. Biol. Chem. 280 (2): 1044–50. doi:10.1074/jbc.M409480200. PMID 15520004.
- ^ Aloj L, Caracò C, Panico M, Zannetti A, Del Vecchio S, Tesauro D, De Luca S, Arra C, Pedone C, Morelli G, Salvatore M (March 2004). "In vitro and in vivo evaluation of 111In-DTPAGlu-G-CCK8 for cholecystokinin-B receptor imaging". J. Nucl. Med. 45 (3): 485–94. PMID 15001692.
- ^ 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". Mol. Pharmacol. 63 (5): 973–82. doi:10.1124/mol.63.5.973. PMID 12695525.
- ^ "Entrez Gene: CCKBR cholecystokinin B receptor". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=887.
- ^ Altar CA, Boyar WC (April 1989). "Brain CCK-B receptors mediate the suppression of dopamine release by cholecystokinin". Brain Res. 483 (2): 321–6. doi:10.1016/0006-8993(89)90176-5. PMID 2706523.
- ^ a b Loonam TM, Noailles PA, Yu J, Zhu JP, Angulo JA (June 2003). "Substance P and cholecystokinin regulate neurochemical responses to cocaine and methamphetamine in the striatum". Life Sci. 73 (6): 727–39. doi:10.1016/S0024-3205(03)00393-X. PMID 12801594.
- ^ Lanza M, Makovec F (January 2000). "Cholecystokinin (CCK) increases GABA release in the rat anterior nucleus accumbens via CCK(B) receptors located on glutamatergic interneurons". Naunyn Schmiedebergs Arch. Pharmacol. 361 (1): 33–8. doi:10.1007/s002109900161. PMID 10651144.
- ^ Dourish CT, O'Neill MF, Coughlan J, Kitchener SJ, Hawley D, Iversen SD (January 1990). "The selective CCK-B receptor antagonist L-365,260 enhances morphine analgesia and prevents morphine tolerance in the rat". Eur. J. Pharmacol. 176 (1): 35–44. doi:10.1016/0014-2999(90)90129-T. PMID 2311658.
- ^ Higgins GA, Sills TL, Tomkins DM, Sellers EM, Vaccarino FJ (August 1994). "Evidence for the contribution of CCKB receptor mechanisms to individual differences in amphetamine-induced locomotion". Pharmacol. Biochem. Behav. 48 (4): 1019–24. doi:10.1016/0091-3057(94)90214-3. PMID 7972279.
- ^ Lu L, Huang M, Ma L, Li J (April 2001). "Different role of cholecystokinin (CCK)-A and CCK-B receptors in relapse to morphine dependence in rats". Behav. Brain Res. 120 (1): 105–10. doi:10.1016/S0166-4328(00)00361-2. PMID 11173090.
- ^ Boyce S, Rupniak NM, Tye S, Steventon MJ, Iversen SD (August 1990). "Modulatory role for CCK-B antagonists in Parkinson's disease". Clin Neuropharmacol 13 (4): 339–47. doi:10.1097/00002826-199008000-00009. PMID 1976438. http://journals.lww.com/clinicalneuropharm/Abstract/1990/08000/Modulatory_Role_for_CCK_B_Antagonists_in.9.aspx.
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.
- 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. PMC 47506. PMID 8415658. //www.ncbi.nlm.nih.gov/pmc/articles/PMC47506/.
- 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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PDB gallery
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1l4t: SOLUTION NMR STRUCTURE OF THE CCK2E3
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Cell surface receptor: G protein-coupled receptors
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Class A:
Rhodopsin like |
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| Class B: Secretin like |
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Orphan
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- GPR (56
- 64
- 97
- 98
- 110
- 111
- 112
- 113
- 114
- 115
- 116
- 123
- 124
- 125
- 126
- 128
- 133
- 143
- 144
- 155
- 157)
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Other
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- Brain-specific angiogenesis inhibitor (1
- 2
- 3)
- Cadherin (1
- 2
- 3)
- Calcitonin
- CALCRL
- CD97
- Corticotropin-releasing hormone (1
- 2)
- EMR (1
- 2
- 3)
- Glucagon (GR
- GIPR
- GLP1R
- GLP2R)
- Growth hormone releasing hormone
- PACAPR1
- GPR
- Latrophilin (1
- 2
- 3
- ELTD1)
- Methuselah-like proteins
- Parathyroid hormone (1
- 2)
- Secretin
- Vasoactive intestinal peptide (1
- 2)
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Class C: Metabotropic
glutamate / pheromone |
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Taste
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- TAS1R (1
- 2
- 3)
- TAS2R (1
- 3
- 4
- 5
- 7
- 8
- 9
- 10
- 13
- 14
- 16
- 19
- 20
- 30
- 31
- 38
- 39
- 40
- 41
- 42
- 43
- 45
- 46
- 50
- 60)
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Other
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- Calcium-sensing receptor
- GABA B (1
- 2)
- Glutamate receptor (Metabotropic glutamate (1
- 2
- 3
- 4
- 5
- 6
- 7
- 8))
- GPRC6A
- GPR (156
- 158
- 179)
- RAIG (1
- 2
- 3
- 4)
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Class F:
Frizzled / Smoothened |
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Frizzled
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- Frizzled (1
- 2
- 3
- 4
- 5
- 6
- 7
- 8
- 9
- 10)
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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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Neuropeptide receptors
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| G protein-coupled receptor |
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Hormone receptors
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Hypothalamic
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CRH · FSH · LHRH · TRH · Somatostatin
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Pituitary
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Vasopressin (1A, 1B, 2) · Oxytocin · LHCG · TSH
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Other
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Atrial natriuretic factor (NPR3) · Calcitonin · Cholecystokinin (A, B) · VIP
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Opioid receptors
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Delta · Kappa · Mu · Nociceptin
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Other neuropeptide receptors
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Angiotensin · Bradykinin (B1, B2) / Tachykinin (TACR1) · Calcitonin gene-related peptide · Galanin · GPCR neuropeptide (B/W, FF, S, Y) · Neurotensin
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| Type I cytokine receptor |
GH · Prolactin
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| Enzyme-linked receptor |
Atrial natriuretic factor (NPR1, NPR2)
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| Other |
Sigma (1, 2)
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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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UpToDate Contents
全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.
English Journal
- Relationship of Genetic Variants With Procedural Pain, Anxiety, and Distress in Children.
- Ersig AL1, Schutte DL2, Standley J3, Leslie E4, Zimmerman B5, Kleiber C6, Hanrahan K6, Murray JC3, McCarthy AM1.
- Biological research for nursing.Biol Res Nurs.2017 May;19(3):339-349. doi: 10.1177/1099800417692878. Epub 2017 Mar 13.
- PMID 28413930
- The Effect of Salt Intake and Potassium Supplementation on Serum Gastrin Levels in Chinese Adults: A Randomized Trial.
- Wang YY1, He WW2, Liu YC3, Lin YF4, Hong LF5.
- Nutrients.Nutrients.2017 Apr 14;9(4). pii: E389. doi: 10.3390/nu9040389.
- PMID 28420122
- Gastrin and Gastric Cancer.
- Smith JP1, Nadella S1, Osborne N2.
- Cellular and molecular gastroenterology and hepatology.Cell Mol Gastroenterol Hepatol.2017 Mar 14;4(1):75-83. doi: 10.1016/j.jcmgh.2017.03.004. eCollection 2017 Jul.
- PMID 28560291
Japanese Journal
- Suppressive Effect on Food Intake of a Potato Extract (Potein【○!R】) Involving Cholecystokinin Release in Rats
- CHEN Wenya,HIRA Tohru,NAKAJIMA Shingo [他],TOMOZAWA Hiroshi,TSUBATA Masahito,YAMAGUCHI Kazuya,HARA Hiroshi
- Bioscience, biotechnology, and biochemistry 76(6), 1104-1109, 2012-06-23
- … The satiating effect of the potato extract was compared in the present study to other protein sources, and the involvement of endogenous cholecystokinin (CCK) secretion was examined. … The suppressive effect on appetite of the potato extract was attenuated by treating with a CCK-receptor antagonist (devazepide). …
- NAID 10030817873
- 腸管での栄養素認識と消化管ホルモン分泌に関する研究:（平成24年度日本栄養・食糧学会奨励賞受賞）
- 比良 徹
- 日本栄養・食糧学会誌 65(5), 215-220, 2012
- 本研究では，腸上皮に散在する消化管内分泌細胞が，管腔内の栄養素を認識して消化管ホルモンを分泌する機構の解明と，食品ペプチドによる消化管ホルモン分泌を介した食欲抑制，血糖上昇抑制の確立を目的とした。膵酵素分泌，満腹感誘導等の作用を持つコレシストキニン（CCK）の分泌機構に関して，カルシウム感知受容体が，フェニルアラニンや各種食品ペプチドの受容体としてCCK分泌に関与することを見いだした。トウモロコシ …
- NAID 130002129275
- 長鎖脂肪酸はG蛋白共役性受容体GPR40を直接刺激してコレシストキニン(CCK)分泌を促進する
- 千葉 勉,Liou Alice P.,Lu Xinping [他]
- Review of gastroenterology & clinical gastroenterology and hepatology 6(2), 3-7, 2011-08-00
- NAID 40018948591
Related Links
- 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 ...
- Learn more about Cholecystokinin B Receptor Gastrointestinal Peptides Celia Chao, Mark R. Hellmich, in Physiology of the Gastrointestinal Tract (Fifth Edition), 2012 6.2.6.7 Regulation of CCK 2 Receptor Expression 2 2 170 2 ...
- Anxiety-related behaviors in cholecystokinin-A, B, and AB receptor gene knockout mice in the plus-maze. the targeted genetic suppression of cholecystokinin B receptor increased the sensitivity of pre- and post-synaptic dopamine
★リンクテーブル★
[★]
- 関
- cholecystokinin B receptor
[★]
- 英
- cholecystokinin B receptor、CCK-B receptor
- 関
- コレシストキニンBレセプター、CCK-B受容体、CCK-Bレセプター
[★]
- 英
- cholecystokinin B receptor、CCK-B receptor
- 関
- コレシストキニンB受容体、CCK-B受容体、CCK-Bレセプター
[★]
- Mg2+存在下でC3, B, Dが反応してC3bBbとなり、これがC3転換酵素(C3bBb)あるいはC5転換酵素(C3bBb3b)を形成する。これらはP(properdin)と結合して活性化し、それぞれC3、C5を活性化する
[★]
コレシストキニン CCK