C-glyco"RGD" as αIIbβ3 and αvβ integrin ligands for imaging applications: Synthesis, in vitro evaluation and molecular modeling.

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 αIIbβ3 and αvβ3 integrins. Molecular-dynamics simulations confirm the suitability of cyclic C-glyco-c(RGDfC) to target αvβ3 integrin. These C-glyco"RGD" could become promising biological tools in particular for Positron Emission Tomography imaging.
PMID: 31371219 [PubMed - as supplied by publisher]

Source: Bioorganic and Medicinal Chemistry - July 24, 2019 Category: Chemistry Authors: Vucko T, Pétry N, Dehez F, Lambert A, Monari A, Lakomy C, Lacolley P, Regnault V, Collet C, Karcher G, Pellegrini-Moïse N, Lamandé-Langle S Tags: Bioorg Med Chem Source Type: research