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

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 foll...

Full description

Saved in:
Bibliographic Details
Published in:ACS medicinal chemistry letters 2020-05, Vol.11 (5), p.857-861
Main Authors: Sanna, Vanna, Youssef, Mohamed Fathy, Pala, Nicolino, Rogolino, Dominga, Carcelli, Mauro, Singh, Pankaj Kumar, Sanchez, Tino, Neamati, Nouri, Sechi, Mario
Format: Article
Language:English
Subjects:
Letter
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.9b00648