Recombinant Human Gastrin/cholecystokinin type B receptor (CCKBR)

CSB-CF004773HU
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20μg
20μg100μg
US$5839
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Express system: in vitro E.coli expression system
Species: Homo sapiens (Human)
Tag Info: N-terminal 10xHis-tagged
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Product Details

Target Names
CCKBR
Uniprot NO.
Species
Homo sapiens (Human)
Source
in vitro E.coli expression system
Expression Region
1-447
Target Protein Sequence
MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITL YAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTF IFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWL LSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGL ISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRS RPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDG PGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRAL PDEDPPTPSIASLSRLSYTTISTLGPG
Protein Length
Full length protein
Tag Info
N-terminal 10xHis-tagged
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Datasheet & COA
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Description

Customer Reviews and Q&A

 Customer Reviews

Target Background

Function
Receptor for gastrin and cholecystokinin. The CCK-B receptors occur throughout the central nervous system where they modulate anxiety, analgesia, arousal, and neuroleptic activity. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.; Isoform 2 is constitutively activated and may regulate cancer cell proliferation via a gastrin-independent mechanism.
Gene References into Functions
  1. We concluded that low serum gastrin is related to increased risk of ER(+) BC development. The results also established that CCKBR/ERK/P65 signaling function is generally tumor suppressive in ER(+) BC, indicating therapies should focus on restoring, not inhibiting, CCKBR/ERK/P65 pathway activity. PMID:30115027
  2. High CCK2R expression is associated with cancer. PMID:26910279
  3. These results suggest that Z-360 exerts an anti-tumor effect through a reduction in anti-apoptosis factors by blocking CCK2R PMID:28739697
  4. High CCK-BR expression is associated with Gastric Cancer. PMID:27518872
  5. There is no identifiable link between nuclear CCK2R expression and all the clinicopathological characteristics examined in a cohort of Taiwanese colon cancer patients. PMID:26508021
  6. Data indicate that variant c.811+32C>A in cholecystokinin-B receptor gene (CCKBR) does not have a significant impact on pancreatic cancer risk or survival in a Hungarian cohort. PMID:26646278
  7. This study showed that CCK2 receptors were highly expressed within the cytoplasmic area of cancerous cells, whereas the levels were very low in normal tissues. PMID:26520651
  8. CCK-BR SNP predicts survival and should be studied as a candidate genetic biomarker for those at risk of pancreatic cancer. PMID:25469546
  9. treatment with gastrin, a CCK2R agonist, stimulated the secretion of GLP-1, and that this effect was likely due to increased expression of proglucagon and PCSK1 (also known as prohormone convertase 3 (PC3 gene)). PMID:25601282
  10. Our results indicate a promoting role of CCK2R on GIST tumourigenesis, particularly in tumours of gastric origin. PMID:22786615
  11. The gastrin receptor is a promising tumor cell surface target for future prostate-cancer-specific imaging applications. PMID:24211650
  12. DeltaFosB induction in prelimbic area occurred selectively in susceptible mice after chronic social defeat stress and produced these effects partly through induction of the cholecystokinin (CCK)-B receptor. PMID:24623766
  13. some CCKBR polymorphisms may contribute to an underlying predisposition towards suicidal behaviour in bipolar disorder. PMID:23890582
  14. Gastric mucosal injury with H. pylori infection destroys the pH barrier on the foveolar epithelium and may induce gastrin receptor expression through pH changes. PMID:23053898
  15. Suggest that CCK2R-mediated COX-2 up-regulation via JAK2/STAT3/PI3K/Akt pathway is involved in the proliferative effect of gastrin on human gastric cancer cells. PMID:23376640
  16. Data suggest that mutations in cholecystokinin 2 receptor (CCK2R) may promote tumorigenesis through deregulated receptor activity and highlight the importance of evaluating CCK2R inhibitors to block both the normal and mutant forms of the receptor. PMID:22516348
  17. These results show the importance of the CCK-BR in regulation of growth and apoptosis in pancreatic cancer. PMID:22442157
  18. A novel splice variant acting as a dominant negative on membrane density of the CCK2R may be of importance for the pathophysiology of certain tumors and for their in vivo CCK2R-targeting. PMID:22040601
  19. A single nucleotide polymorphism in the cholecystokinin-B receptor that alters splicing predicts survival in pancreatic cancer. PMID:22277584
  20. proximal DNA elements within the human gastrin gene promoter mediate interactions between JunD, which induces gastrin gene expression and menin, which suppresses JunD-mediated activation. PMID:21852362
  21. Genetic polymorphisms in cholecystokinin B receptor may play a role in antipsychotic induced weight gain in schizophrenia patients. PMID:20732371
  22. Regulation of membrane cholecystokinin-2 receptor by agonists enables classification of partial agonists as biased agonists. PMID:21156802
  23. a positive-feedback loop whereby gastrin, acting via the CCK2 receptor, increases its own expression PMID:20932834
  24. The CCK(2)splice variant with retention of intron 4 (Ri4sv) is a marker of specific gastrointestinal and lung tumours. PMID:19627395
  25. The cholecystokinin 2 receptor allele with 21 CT repeats was associated with multiple chemical sensitivity when compared in post hoc analyses with all individuals from the population sample. PMID:20185366
  26. Results show that signaling through ACAT/cholesterol esterification is a novel pathway for the CCK2R that contributes to tumor cell proliferation and invasion. PMID:19502590
  27. Expression of gastrin and cholecystokinin 2 (CCK(2)) receptor splice variants are upregulated in human colonic adenomas where they are thought to contribute to tumor growth and progression. PMID:19697327
  28. A misspliced form of the cholecystokinin-B/gastrin receptor in pancreatic carcinoma: role of reduced sellular U2AF35 and a suboptimal 3'-splicing site leading to retention of the fourth intron. PMID:11830556
  29. hGARE is proposed as a new candidate target gene in microsatellite instability tumorigenesis. PMID:11896205
  30. role in activating protein kinase D2 PMID:12058027
  31. Hyper-gastrinaemia may promote proliferation of human colonic adenomas that expressnon-truncated CCK-2 receptor isoforms. PMID:12189558
  32. data represent the first evidence for role in regulating cell-cell and cell-substrate adhesion and support a role in the progression of carcinoma PMID:12400008
  33. data support the hypothesis that cholecystokinin-B receptor mediated activation of the hypothalamic-pituitary-adrenal axis is relatively resistant to cortisol feedback inhibition PMID:12510010
  34. induction by oncogenic ras in LoVo and Colo320HSR colon cancer cell lines PMID:12761477
  35. Cholecystokinin-A receptor and B receptor polymorphisms, considered alone, showed no correlation with hallucinations in Parkinson's disease PMID:12777967
  36. this is the first report that provides evidence for the high tumorigenic effect of a constitutively active CCK2R mutant, thus raising a potential role of the CCK2R in human cancer. PMID:12955087
  37. findings suggest physiological functions for the CCK(2)R in calcitonin-secretion and gene expression as well as a pathophysiological role in medullary thyroid carcinoma proliferation PMID:14759564
  38. CCK exerts secretagogue action on human ZG cells, acting through CCK2-Rs coupled to the adenylate cyclase/protein kinase A signaling cascade PMID:15001623
  39. A role is implicated for the CCKB receptor gene in suicide completers, the highest gene expression being observed in the cerebellum followed by cingulate gyrus and pre-frontal cortex compared to their age and sex-matched controls. PMID:15036586
  40. Gastrin/CCK-B receptor autocrine or paracrine pathway may possibly play an important role in the progression of gastric cancer. PMID:15040018
  41. CCK2i4svR, a splice variant of cholecystokinin-2 receptor, has a role in agonist-independent activation of Src tyrosine kinase PMID:15292208
  42. Findings are consistent with the notion that genetic variation in the CCK B receptor neurotransmitter system contributes to the pathogenesis of panic disorder. PMID:15354400
  43. the MEK1/ERK1/2 pathway couples the CCK2 receptor to nuclearization and DNA binding of Egr-1 PMID:15611055
  44. analysis of interspecies polymorphism in the human and rat cholecystokinin receptor-2 and its effect on the cholecystokinin binding site PMID:15817487
  45. Photoaffinity labeling of the type B CCK receptor provides evidence for the peptide-binding domain to include receptor loop and amino-terminal tail regions residing at the extracellular surface of the plasma membrane. PMID:15850403
  46. human normal, inflammatory, and malignant gastric tissues simultaneously express the classical and alternative splicing cholecystokinin-B/gastrin receptor genes PMID:15989082
  47. Study confirms that a high proportion of gastric cancer tissue samples express the gastrin/CCKB receptor, which can stimulate the growth of gastrin/CCKB receptor-positive gastric cancer cells. PMID:16012719
  48. CCK2 gastrin receptor may have a role in leukemia PMID:16142371
  49. Gastrin exerts an antiproliferative and proapoptotic effect on human colon cancer cells expressing the wild-type CCK2 receptor. PMID:16143134
  50. The expression rates of gastrin and gastrin receptor are high (about a half) in gastric carcinoma tissues, and there is an association between gastrin and gastrin receptor expression. PMID:16228228

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Subcellular Location
Cell membrane; Multi-pass membrane protein.
Protein Families
G-protein coupled receptor 1 family
Tissue Specificity
Isoform 1 is expressed in brain, pancreas, stomach, the colon cancer cell line LoVo and the T-lymphoblastoma Jurkat, but not in heart, placenta, liver, lung, skeletal muscle, kidney or the stomach cancer cell line AGS. Expressed at high levels in the smal
Database Links

HGNC: 1571

UNIGENE: Hs.203

KEGG: hsa:887

STRING: 9606.ENSP00000335544

OMIM: 118445

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