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