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.
Inhibition of Human Immunodeficiency Virus-1 Integrase by β-Diketo Acid Coated Gold Nanoparticles / Sanna, V.; Youssef, M. F.; Pala, N.; Rogolino, D.; Carcelli, M.; Singh, P. K.; Sanchez, T.; Neamati, N.; Sechi, M.. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - 11:5(2020), pp. 857-861. [10.1021/acsmedchemlett.9b00648]
Inhibition of Human Immunodeficiency Virus-1 Integrase by β-Diketo Acid Coated Gold Nanoparticles
Sanna V.;Pala N.;Sechi M.
2020-01-01
Abstract
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
