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CCK receptors and cancer

Graham S Baldwin1, Arthur Shulkes

  • 1University of Melbourne Department of Surgery, Austin Health, Melbourne, Victoria, Australia. grahamsb@unimelb.edu.au

Current Topics in Medicinal Chemistry
|June 23, 2007
PubMed

Insights

Cholecystokinin (CCK) receptors are found in neural and neuroendocrine tumors, but not widely in gastrointestinal cancers. CCK-2 receptors may still play a role in esophageal and gastric cancer development.

Area of Science:

  • Gastroenterology
  • Oncology
  • Molecular Biology

Background:

  • Cholecystokinin (CCK) receptors have been investigated for their role in gastrointestinal cancers.
  • Initial findings of CCK-1 and CCK-2 receptor mRNA in tumors were promising but later tempered by restricted protein expression.

Purpose of the Study:

  • To review the expression patterns of CCK receptors in gastrointestinal cancers.
  • To explore the potential role of CCK-2 receptors in esophageal and gastric adenocarcinomas.
  • To discuss therapeutic strategies involving CCK receptors for cancer treatment.

Main Methods:

  • Review of existing literature on CCK receptor expression in gastrointestinal tumors.
  • Analysis of receptor autoradiography data for CCK-2 receptors in medullary thyroid carcinomas.
  • Examination of in vitro and animal model data regarding CCK-2 receptor function in cancer development.

Main Results:

  • CCK-1 and CCK-2 receptor protein expression is primarily restricted to tumors of neural or neuroendocrine origin.
  • Over 90% of medullary thyroid carcinomas exhibit CCK-2 receptor expression.
  • CCK receptors are generally absent in most gastrointestinal adenocarcinomas.

Conclusions:

  • Despite limited expression in many gastrointestinal adenocarcinomas, the CCK-2 receptor may contribute to esophageal and gastric cancer development.
  • Further research is warranted to elucidate the role of CCK-2 receptors in these cancers.
  • Therapeutic strategies include radiolabeled gastrin/CCK derivatives for imaging and selective antagonists for treatment of CCK receptor-expressing tumors.

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