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Inhibition of Human Immunodeficiency Virus‑1 Integrase by β‑Diketo Acid Coated Gold Nanoparticles

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journal contribution
posted on 2020-03-25, 14:38 authored by Vanna Sanna, Mohamed Fathy Youssef, Nicolino Pala, Dominga Rogolino, Mauro Carcelli, Pankaj Kumar Singh, Tino Sanchez, Nouri Neamati, Mario Sechi
Gold nanoparticles (GNPs) have been proposed as carriers for drugs to improve their intrinsic therapeutic activities and to overcome pharmacokinetic problems. In this study, novel nanosystems constituted by a model β-diketo acid (DKA) grafted to the surface of GNPs were designed and synthesized following the “multivalent high-affinity” binding strategy. These first nanoscale DKA prototypes showed improved inhibition of HIV-1 integrase (HIV-1 IN) catalytic activities as compared with free DKA ligands.

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