PMID- 32435396 OWN - NLM STAT- PubMed-not-MEDLINE LR - 20210514 IS - 1948-5875 (Print) IS - 1948-5875 (Electronic) IS - 1948-5875 (Linking) VI - 11 IP - 5 DP - 2020 May 14 TI - Inhibition of Human Immunodeficiency Virus-1 Integrase by beta-Diketo Acid Coated Gold Nanoparticles. PG - 857-861 LID - 10.1021/acsmedchemlett.9b00648 [doi] AB - 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. CI - Copyright (c) 2020 American Chemical Society. FAU - Sanna, Vanna AU - Sanna V AD - Nanomater s.r.l., c/o Porto Conte Ricerche, Alghero, Italy. FAU - Youssef, Mohamed Fathy AU - Youssef MF AD - Department of Chemistry and Pharmacy, Laboratory of Drug Design and Nanomedicine, University of Sassari, 07100 Sassari, Italy. FAU - Pala, Nicolino AU - Pala N AD - Department of Chemistry and Pharmacy, Laboratory of Drug Design and Nanomedicine, University of Sassari, 07100 Sassari, Italy. FAU - Rogolino, Dominga AU - Rogolino D AD - Department of Chemistry, Life Sciences and Environmental Sustainability, University of Parma, Parco Area delle Scienze, 43121 Parma, Italy. FAU - Carcelli, Mauro AU - Carcelli M AD - Department of Chemistry, Life Sciences and Environmental Sustainability, University of Parma, Parco Area delle Scienze, 43121 Parma, Italy. FAU - Singh, Pankaj Kumar AU - Singh PK AD - Department of Chemistry and Pharmacy, Laboratory of Drug Design and Nanomedicine, University of Sassari, 07100 Sassari, Italy. FAU - Sanchez, Tino AU - Sanchez T AD - National Center for Advancing Translational Sciences - NIH, Rockville, Maryland 20850, United States. FAU - Neamati, Nouri AU - Neamati N AD - Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109, United States. FAU - Sechi, Mario AU - Sechi M AD - Department of Chemistry and Pharmacy, Laboratory of Drug Design and Nanomedicine, University of Sassari, 07100 Sassari, Italy. LA - eng PT - Journal Article DEP - 20200320 PL - United States TA - ACS Med Chem Lett JT - ACS medicinal chemistry letters JID - 101521073 PMC - PMC7236234 COIS- The authors declare no competing financial interest. EDAT- 2020/05/22 06:00 MHDA- 2020/05/22 06:01 PMCR- 2021/05/14 CRDT- 2020/05/22 06:00 PHST- 2019/12/24 00:00 [received] PHST- 2020/03/20 00:00 [accepted] PHST- 2020/05/22 06:00 [entrez] PHST- 2020/05/22 06:00 [pubmed] PHST- 2020/05/22 06:01 [medline] PHST- 2021/05/14 00:00 [pmc-release] AID - 10.1021/acsmedchemlett.9b00648 [doi] PST - epublish SO - ACS Med Chem Lett. 2020 Mar 20;11(5):857-861. doi: 10.1021/acsmedchemlett.9b00648. eCollection 2020 May 14.