Abstract |
Over the past 20 years there has been considerable interest in the role of CCK receptors in gastrointestinal cancer. Initial excitement over reports of the detection by PCR of CCK-1 and CCK-2 receptor mRNA in a wide range of gastrointestinal tumours has been tempered by the realisation that the presence of receptor binding sites is much more restricted. The current consensus is that expression of CCK-1 and -2 receptor proteins is common only in tumours of neural or neuroendocrine origin. A striking example of this general rule has been provided by the detection of CCK-2 receptors by receptor autoradiography in more than 90% of medullary thyroid carcinomas. Despite the absence of CCK receptors from many gastrointestinal adenocarcinomas, evidence from animal models and from tumour cell lines in vitro suggests that the CCK-2 receptor may contribute to the development of esophageal and gastric adenocarcinomas, and further experimental work in these areas is clearly warranted. Promising therapeutic approaches include the development of radiolabelled gastrin/CCK derivatives for use in tumour imaging, and the use of appropriate selective antagonists for treatment of those tumour subtypes likely to express CCK receptors.
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Authors | Graham S Baldwin, Arthur Shulkes |
Journal | Current topics in medicinal chemistry
(Curr Top Med Chem)
Vol. 7
Issue 12
Pg. 1232-8
( 2007)
ISSN: 1873-4294 [Electronic] United Arab Emirates |
PMID | 17584144
(Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't, Review)
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Chemical References |
- Receptors, Cholecystokinin
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Topics |
- Animals
- Gastrointestinal Neoplasms
(genetics, metabolism, pathology, therapy)
- Humans
- Pancreatic Neoplasms
(genetics, metabolism, pathology, therapy)
- Receptors, Cholecystokinin
(chemistry, genetics, metabolism)
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