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Inhibition of Human Immunodeficiency Virus-1 Integrase by β-Diketo Acid Coated Gold Nanoparticles.
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-03-20 , DOI: 10.1021/acsmedchemlett.9b00648 Vanna Sanna 1 , Mohamed Fathy Youssef 2 , Nicolino Pala 2 , Dominga Rogolino 3 , Mauro Carcelli 3 , Pankaj Kumar Singh 2 , Tino Sanchez 4 , Nouri Neamati 5 , Mario Sechi 2
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-03-20 , DOI: 10.1021/acsmedchemlett.9b00648 Vanna Sanna 1 , Mohamed Fathy Youssef 2 , Nicolino Pala 2 , Dominga Rogolino 3 , Mauro Carcelli 3 , Pankaj Kumar Singh 2 , Tino Sanchez 4 , Nouri Neamati 5 , Mario Sechi 2
Affiliation
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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.
中文翻译：
β-二酮酸包被的金纳米粒子对人免疫缺陷病毒1整合酶的抑制作用。
金纳米颗粒（GNP）已被提议作为药物的载体，以改善其内在的治疗活性并克服药代动力学问题。在这项研究中，按照“多价高亲和力”结合策略设计和合成了由模型β-二酮酸（DKA）嫁接到GNP表面构成的新型纳米系统。与游离的DKA配体相比，这些首批纳米级DKA原型显示出对HIV-1整合酶（HIV-1 IN）催化活性的抑制作用得到改善。
更新日期：2020-03-20
中文翻译：
β-二酮酸包被的金纳米粒子对人免疫缺陷病毒1整合酶的抑制作用。
金纳米颗粒（GNP）已被提议作为药物的载体，以改善其内在的治疗活性并克服药代动力学问题。在这项研究中，按照“多价高亲和力”结合策略设计和合成了由模型β-二酮酸（DKA）嫁接到GNP表面构成的新型纳米系统。与游离的DKA配体相比，这些首批纳米级DKA原型显示出对HIV-1整合酶（HIV-1 IN）催化活性的抑制作用得到改善。
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