Design of peptide vectors through chemoselective ligations - Archive ouverte HAL
Communication Dans Un Congrès Année : 2020

Design of peptide vectors through chemoselective ligations

Résumé

The identification of molecular markers that can differentiate a tumor from healthy tissue is essential for the development of more successful diagnostic methods and more effective antitumoral agents. Integrins such as αVβ3 are attractive therapeutic targets as these receptors are cell surface proteins that are highly expressed on tumor microenvironment. A characteristic feature of this receptor is its high binding affinity for the ubiquitous triad sequence arginine-glycine-aspartic acid (RGD). The design of numerous RGD-containing cyclopeptides has led to highly selective synthetic ligands with enhanced binding affinities.1 We have shown that clustered RGD-containing compounds offer an interesting outlook for biological applications. These compounds are based on a cyclic decapeptide scaffold containing two independent functional domains: (I) a clustered ligand domain and (II) an effector domain for supplementary function. Access to such biomolecular compounds may become a challenging task. We recently developed methodologies using chemoselective ligations to achieve sophisticated macromolecules 2 with desirable biological properties such as tumor imaging, drug delivery and cell capture.3 ____ [1] M. Pfaff, K. Tangemann, B. Müller, M. Gurrath, G. Müller, H. Kessler, R. Timpl and J. Engel, J. Biol. Chem. 1994, 269, 20233 ; W. Arap, R. Pasqualini and E. Ruoslahti, Science 1998, 279, 377. [2] M. Galibert, O. Renaudet, P. Dumy, and D. Boturyn, Angew. Chem. Int. Ed. 2011, 50, 1901. [3] C. H. F. Wenk, F. Ponce, S. Guillermet, C. Tenaud, D. Boturyn, et al., Cancer Lett. 2013, 334, 188 ; A. Karageorgis, M. Claron, R. Jugé, C. Aspord, C. Leloup, et al., Mol. Ther. 2017, 25, 534 ; M. Degardin, D. Thakar, M. Claron, R. P. Richter, L. Coche-Guérente and D. Boturyn. J. Mat. Chem. B 2017, 5, 4745.

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Chimie
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Dates et versions

hal-04746917 , version 1 (21-10-2024)

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  • HAL Id : hal-04746917 , version 1

Citer

Didier Boturyn. Design of peptide vectors through chemoselective ligations. 4ème journée Ligation Chimique, Jan 2020, Orléans, France. ⟨hal-04746917⟩

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