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Synthèse par ingénierie moléculaire de vecteurs peptidiques pour des applications anticancéreuses

Abstract : The cancer research focuses on the development of "targeted strategies" by increasing therapeutic efficacy and reducing toxicity. In this context, this work has been devoted to the design of peptide vectors for anticancer applications. These systems have been developed using a cyclodecapeptide scaffold which presents specific conformational properties. Two different approaches were considered. The first one was to investigate new tumor receptor ligands based on the recognition domain of a therapeutics monoclonal antibody. We propose the design of Rituximab mimics which targets the CD20 antigen used for the treatment of Non-Hodkinien lymphoma. In the second approach, we developed vectors for tumor imaging. For this purpose, multivalent scaffolds containing RGD peptide that target integrin alpha-v-beta-3 were combined with several detection elements and evaluated by using PET, MRI and optical imaging techniques. In both strategies, delivery systems consist of a recognition domain bearing one or more ligands and an effector module consisting of an active element, both assembled on the molecular scaffold. Therefore, we developed procedures for biomolecular assemblies by modulating the grafting sites on scaffold. We have thendeveloped synthetic methodologies combining several orthogonal chemoselective ligations. We demonstrate that this strategy offers many benefits and enables macromolecular assemblies in one step without intermediate purification or deprotection.
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Contributor : Mathieu Galibert <>
Submitted on : Thursday, December 16, 2010 - 6:51:23 PM
Last modification on : Friday, November 6, 2020 - 3:45:54 AM
Long-term archiving on: : Monday, November 5, 2012 - 2:30:18 PM


  • HAL Id : tel-00547615, version 1




Mathieu Galibert. Synthèse par ingénierie moléculaire de vecteurs peptidiques pour des applications anticancéreuses. Chimie. Université Joseph-Fourier - Grenoble I, 2010. Français. ⟨tel-00547615⟩



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