Gastrin receptor pharmacology

被引：26

作者：

Graham J. Dockray

Andy Moore

Andrea Varro

D. Mark Pritchard

机构：

[1] Departments of Cell and Molecular Physiology, Institute of Translational Medicine, University of Liverpool, Liverpool

[2] Gastroenterology, Institute of Translational Medicine, University of Liverpool, Liverpool

[3] Physiological Laboratory, Institute of Translational Medicine, University of Liverpool, Liverpool L69 3BX, Crown St

来源：

Current Gastroenterology Reports | 2012年 / 14卷 / 6期

关键词：

Acid secretion; CCK2; receptor; Cell migration; Cholecystokinin; Colon cancer; Enterochromaffin-like cell; Gastric cancer; Gastrin; Gastrin/cholecystokinin-B receptor; Lung cancer; Neuroendocrine tumour; Oesophageal cancer; Pancreatic cancer; Parietal cell; Proliferation; Thyroid medullary cancer; Tumour imaging;

D O I：

10.1007/s11894-012-0293-1

中图分类号：

学科分类号：

摘要：

C-Terminally amidated gastrins act at cholecystokinin-2 receptors (CCK2R), which are normally expressed by gastric parietal and enterochromaffin-like (ECL) cells and smooth muscle; there is also extensive expression in the CNS where the main endogenous ligand is cholecystokinin. A variety of neoplasms express CCK2R, or splice variants, including neuroendocrine, pancreatic, medullary thyroid and lung cancers. Other products of the gastrin gene (progastrin, the Gly-gastrins) may stimulate cell proliferation but are not CCK2R ligands. Depending on the cell type, stimulation of CCK2R evokes secretion, increases proliferation and cell migration, inhibits apoptosis, and controls the expression of various genes. These effects are mediated by increased intracellular calcium and activation of protein kinase C, MAPkinase and other protein kinase cascades. There has been recent progress in developing CCK2R ligands that can be used for imaging tumours expressing the receptor. New antagonists have also been developed, and there is scope for using these for suppression of gastric acid and for treatment of neuroendocrine and other CCK2R-expressing tumours. © Springer Science+Business Media, LLC 2012. © Springer Science+Business Media, LLC 2012.

引用

页码：453 / 459

页数：6

共 65 条

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