Nastorazepide is a selective, orally available antagonist of gastrin/cholecystokinin 2 (CCK-2) receptor with potential antineoplastic activity.
靶点:
cholecystokinin
体外研究:
Nastorazepide binds to the gastrin/CCK-2 receptor, thereby preventing receptor activation by gastrin, a peptide hormone frequently associated with the proliferation of gastrointestinal and pancreatic tumor cells
体内研究:
Nastorazepide significantly inhibits the growth of subcutaneous xenografts of human pancreatic tumor cells in mice, and that Nastorazepide combined with gemcitabine prolonged survival in a pancreatic carcinoma orthotopic xenograft mice
参考文献:
1. Kato H, et al. CCK-2/gastrin receptor signaling pathway is significant for gemcitabine-induced gene expression of VEGF in pancreatic carcinoma cells. Life Sci. 2011 Oct 24;89(17-18):603-8.