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Quantifying Agonist Activity at G Protein-coupled Receptors

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Published on: December 26, 2011

Gastrin receptor pharmacology.

Graham J Dockray¹, Andy Moore, Andrea Varro

¹Departments of Cell and Molecular Physiology, Institute of Translational Medicine, University of Liverpool, Liverpool, UK. g.j.dockray@liverpool.ac.uk

Current Gastroenterology Reports

|September 18, 2012

Summary

C-terminally amidated gastrins activate cholecystokinin-2 receptors (CCK2R), which are implicated in various cancers. New CCK2R ligands show promise for tumor imaging and therapeutic applications.

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Published on: September 18, 2014

Area of Science:

Gastroenterology and Oncology
Molecular Biology
Pharmacology

Background:

Cholecystokinin-2 receptors (CCK2R) are activated by amidated gastrins and expressed in gastric cells, smooth muscle, and the central nervous system (CNS).
CCK2R and its splice variants are also found in various neoplasms, including neuroendocrine, pancreatic, medullary thyroid, and lung cancers.
Other gastrin gene products, like progastrin and Gly-gastrins, may influence cell proliferation but do not bind to CCK2R.

Purpose of the Study:

To investigate the role of CCK2R in normal physiology and cancer.
To explore the therapeutic potential of CCK2R ligands for cancer diagnosis and treatment.

Main Methods:

Review of existing literature on gastrin, CCK2R expression, and signaling pathways.
Analysis of the development of CCK2R ligands for imaging and therapeutic applications.

Main Results:

CCK2R stimulation by gastrins influences cellular secretion, proliferation, migration, apoptosis, and gene expression via intracellular calcium and protein kinase cascades.
CCK2R is expressed in a range of tumors, making it a potential target for cancer therapy.
Progress has been made in developing CCK2R ligands for tumor imaging and novel antagonists for therapeutic use.

Conclusions:

CCK2R plays a significant role in both normal cellular functions and the pathogenesis of various cancers.
CCK2R-targeting agents, including imaging ligands and antagonists, offer promising avenues for the diagnosis and treatment of CCK2R-expressing tumors and other conditions like gastric acid suppression.