Side chain effect in the modulation of α_vβ₃/α₅β₁ integrin activity via clickable isoxazoline-RGD-mimetics: development of molecular delivery systems.

ABSTRACT: Construction of small molecule ligand (SML) based delivery systems has been performed starting from a polyfunctionalized isoxazoline scaffold, whose α_vβ₃ and α₅β₁ integrins' potency has been already established. The synthesis of this novel class of ligands was obtained by conjugation of linkers to the heterocyclic core via Huisgen-click reaction, with the aim to use them as "shuttles" for selective delivery of diagnostic agents to cancer cells, exploring the effects of the side chains in the interaction with the target. Compounds 17b and 24 showed excellent potency towards α₅β₁ integrin acting as selective antagonist and agonist respectively. Further investigations confirmed their effects on target receptor through the analy

SUBMITTER: Ferrazzano L 

PROVIDER: S-EPMC7198601 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature