Synthesis and evaluation of cholecystokinin trimers: a multivalent approach to pancreatic cancer detection and treatment

Bioorg Med Chem Lett. 2013 Apr 15;23(8):2422-5. doi: 10.1016/j.bmcl.2013.02.022. Epub 2013 Feb 13.

Abstract

In the quest for novel tools for early detection and treatment of cancer, we propose the use of multimers targeting overexpressed receptors at the cancer cell surface. Indeed, multimers are prone to create multivalent interactions, more potent and specific than their corresponding monovalent versions, thus enabling the potential for early detection. There is a lack of tools for early detection of pancreatic cancer, one of the deadliest forms of cancer, but CCK2-R overexpression on pancreatic cancer cells makes CCK based multimers potential markers for these cells. In this Letter, we describe the synthesis and evaluation of CCK trimers targeting overexpressed CCK2-R.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biomarkers, Tumor / biosynthesis
  • Biomarkers, Tumor / chemistry
  • Cholecystokinin / analogs & derivatives*
  • Cholecystokinin / chemical synthesis*
  • Cholecystokinin / chemistry
  • Humans
  • Pancreatic Neoplasms / diagnosis
  • Pancreatic Neoplasms / drug therapy
  • Pancreatic Neoplasms / metabolism*
  • Receptors, Cholecystokinin / biosynthesis
  • Receptors, Cholecystokinin / chemistry
  • Receptors, Cholecystokinin / metabolism

Substances

  • Biomarkers, Tumor
  • Receptors, Cholecystokinin
  • Cholecystokinin