Synthesis and evaluation of cholecystokinin trimers: A multivalent approach to pancreatic cancer detection and treatment |
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| Authors: | Nabila Brabez Kevin L. Nguyen Kara Saunders Ryan Lacy Liping Xu Robert J. Gillies Ronald M. Lynch Gerard Chassaing Solange Lavielle Victor J. Hruby |
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| Affiliation: | 1. UPMC Paris 06, UMR 7203, Laboratoire des BioMolécules, Université P. et M. Curie, 75005 Paris, France;2. CNRS, UMR 7203, France;3. ENS, UMR 7203, Département de Chimie, Ecole Normale Supérieure, 75005 Paris, France;4. University of Arizona, Department of Chemistry and Biochemistry, Tucson, AZ 85721, USA;5. H. Lee Moffitt Cancer Center and Research Institute, Department of Cancer Imaging and Metabolism, Tampa, FL 33612, USA;6. University of Arizona, Department of Physiology, Tucson, AZ 85721, USA |
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| 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. |
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