1. C-glyco"RGD" as α IIb β 3 and α v β integrin ligands for imaging applications: Synthesis, in vitro evaluation and molecular modeling.
- Author
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Vucko T, Pétry N, Dehez F, Lambert A, Monari A, Lakomy C, Lacolley P, Regnault V, Collet C, Karcher G, Pellegrini-Moïse N, and Lamandé-Langle S
- Subjects
- Humans, Models, Molecular, Integrin alphaVbeta3 metabolism, Ligands
- Abstract
The design of conjugates displaying simultaneously high selectivity and high affinity for different subtypes of integrins is a current challenge. The arginine-glycine-aspartic acid amino acid sequence (RGD) is one of the most efficient short peptides targeting these receptors. We report herein the development of linear and cyclic fluoro-C-glycoside"RGD" conjugates, taking advantage of the robustness and hydrophilicity of C-glycosides. As attested by in vitro evaluation, the design of these C-glyco"RGD" with a flexible three-carbon triazolyl linker allows distinct profiles towards α
IIb β3 and αv β3 integrins. Molecular-dynamics simulations confirm the suitability of cyclic C-glyco-c(RGDfC) to target αv β3 integrin. These C-glyco"RGD" could become promising biological tools in particular for Positron Emission Tomography imaging., (Copyright © 2019 Elsevier Ltd. All rights reserved.)- Published
- 2019
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