Regular ArticleA Truncated Isoform of Human CCK-B/Gastrin Receptor Generated by Alternative Usage of a Novel Exon
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Gastrin
2013, Handbook of Biologically Active PeptidesGastrointestinal Peptides: Gastrin, Cholecystokinin, Somatostatin, and Ghrelin. Gastrin, Cholecystokinin, Somatostatin, and Ghrelin
2012, Physiology of the Gastrointestinal Tract, Two Volume SetCharacterization of a novel five-transmembrane domain cholecystokinin-2 receptor splice variant identified in human tumors
2012, Molecular and Cellular EndocrinologyCitation Excerpt :However, these data are still controversial since abundance of variant transcript in colorectal cancers as well as its constitutive activity were not always confirmed (Cheng et al., 2005; Korner et al., 2010). Two other CCK2R transcript variants, isolated from gastric cancer cells and colorectal cancers were described (Miyake, 1995; Schmitz et al., 2001). The demonstration of the clinical relevance of the expression of ΔE2-CCK2R in human tumors will require further investigations on a large series of tumor samples as our current study used a highly heterogeneous series of samples with only few cases per tumor type and thus could not permit a meaningful correlative evaluation with any kind of clinical parameters.
Gastrointestinal Peptides: Gastrin, Cholecystokinin, Somatostatin, and Ghrelin
2012, Physiology of the Gastrointestinal TractDifferential sensitivity of types 1 and 2 cholecystokinin receptors to membrane cholesterol
2012, Journal of Lipid ResearchCitation Excerpt :To determine the possible structural basis for differential cholesterol sensitivity of these receptors, we began by utilizing a series of chimeric receptors (CCK2R/CCK1R) originally prepared and characterized by Wu et al. (17). These chimeric constructs take advantage of the fact that the genes encoding human CCK1R and CCK2R each contain five exons in a similar organization (17, 32–34). The exons from CCK1R were sequentially replaced by exons from CCK2R, starting from the N terminus.
Targeting gastrin for the treatment of gastric acid related disorders and pancreatic cancer
2011, Trends in Pharmacological SciencesCitation Excerpt :In addition, CCK2 receptor expression and/or gastrin binding has been demonstrated in clinical samples from several gastrointestinal cancers including colorectal, gastric and pancreatic cancers [45–47]. However, the identification of additional CCK2 receptor isoforms (truncated CCK2 receptor, [48]; CCK2S and CCK2L; [49] and CCKBri4sv, [50]) has resulted in some speculation over the possibility that the neoplastic effects of gastrin (and its multiple molecular forms) could be mediated by an alternative CCK2 receptor [51]. The clinical pharmacological relevance of the existence of additional CCK2 receptor subtypes remains unclear as only small differences in antagonist affinity values have been reported between the different isoforms studied to date [52].