Inhibition of Human Immunodeficiency Virus-1 Integrase by beta-Diketo Acid Coated Gold Nanoparticles

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作   者：

Sanna, Vanna;  Youssef, Mohamed Fathy;  Pala, Nicolino;  Rogolino, Dominga;  Carcelli, Mauro;  Singh, Pankaj Kumar;  Sanchez, Tino;  Neamati, Nouri;  Sechi, Mario; 

作者机构：

Rockville;  Natl Ctr Adv Translat Sci;  Dept Med Chem;  I-07100 Sassari;  Alghero;  Univ Sassari;  I-43121 Parma;  Dept Chem Life Sci & Environm Sustainabil;  Dept Chem & Pharm;  Coll Pharm;  MI 48109 USA;  Univ Michigan;  Lab Drug Design & Nanomed;  NIH;  Univ Parma;  Ann Arbor;  Nanomater Srl;  Italy;  MD 20850 USA; 

关键词：

gold nanoparticles;  multivalent ligands;  beta-diketo acids;  HIV-1 integrase inhibitors; 

期刊名称：

ACS medicinal chemistry letters

i s s n：

1948-5875

年卷期：

2020 年 11 卷 5 期

页   码：

857-861

页   码：

摘   要：

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 beta-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.