2016
DOI: 10.3892/or.2016.4588
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Abstract: Abstract. Colon and pancreatic cancers contribute to 90,000 deaths each year in the USA. These cancers lack targeted therapeutics due to heterogeneity of the disease and multiple causative factors. One important factor that contributes to increased colon and pancreatic cancer risk is gastrin. Gastrin mediates its actions through two G-protein coupled receptors (GPCRs): cholecystokinin receptor A (CCK-A) and CCK-B/gastrin receptor. Previous studies have indicated that colon cancer predominantly expresses CCK-A … Show more

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Cited by 7 publications
(10 citation statements)
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References 35 publications
(28 reference statements)
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“…Both agents inhibited tumour growth significantly from the day treatment was initiated and maintained the growth inhibitory properties until sacrifice ( Figure 10) Overall, it was clearly shown, that colon and pancreatic cancers response to CCK 1 antagonists and not CCK 2 antagonists [29]. We agree, it is unlikely that, gastrin is more important in pancreatic cancer than cholecystokinin.…”
Section: Pancreatic Cancer Xenograft Study Miapaca Tumourmentioning
confidence: 76%
See 2 more Smart Citations
“…Both agents inhibited tumour growth significantly from the day treatment was initiated and maintained the growth inhibitory properties until sacrifice ( Figure 10) Overall, it was clearly shown, that colon and pancreatic cancers response to CCK 1 antagonists and not CCK 2 antagonists [29]. We agree, it is unlikely that, gastrin is more important in pancreatic cancer than cholecystokinin.…”
Section: Pancreatic Cancer Xenograft Study Miapaca Tumourmentioning
confidence: 76%
“…Overall, the introduction of alkyl groups, most preferred an isobutyl-group, provided a CCK 1 selective antagonist a hydroxylpyrrolone 9, which was the selected development candidate PNB-028 for colon and pancreatic cancer associated with the CCK C receptor [29].…”
Section: Sar Optimisationmentioning
confidence: 99%
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“…MAC16 is resistant to alkylating agents and has a high expression of the CCK receptor In line with the receptor expression, activity was found for lactame 7 and 9, but the IC 50 for benzylated lactame. 32,33 19 was 4 times higher. Previously we reported activity for lactame 9 on pancreatic cancer cell lines.…”
Section: Cell Based In Vitro Assaymentioning
confidence: 87%
“…Overall, the introduction of alkyl groups, most preferred an isobutylgroup, provided a CCK 1 selective antagonist PNB-081, which was the selected development candidate. A fluorinated analogue had potent anticancer properties via the CCKC receptor [38]. The phenyl-ethyl hydroxyl-pyrolone, lactam20=PNB-001 is CCK 2 / gastrin selective antagonist, outlined in (Figure 2).…”
Section: Sar Optimisationmentioning
confidence: 99%