β-二酮酸包被的金纳米颗粒对人免疫缺陷病毒1型整合酶的抑制作用
Inhibition of Human Immunodeficiency Virus-1 Integrase by β-Diketo Acid Coated Gold Nanoparticles.
作者信息
Sanna Vanna, Youssef Mohamed Fathy, Pala Nicolino, Rogolino Dominga, Carcelli Mauro, Singh Pankaj Kumar, Sanchez Tino, Neamati Nouri, Sechi Mario
机构信息
Nanomater s.r.l., c/o Porto Conte Ricerche, Alghero, Italy.
Department of Chemistry and Pharmacy, Laboratory of Drug Design and Nanomedicine, University of Sassari, 07100 Sassari, Italy.
出版信息
ACS Med Chem Lett. 2020 Mar 20;11(5):857-861. doi: 10.1021/acsmedchemlett.9b00648. eCollection 2020 May 14.
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.
摘要
金纳米颗粒（GNPs）已被提议作为药物载体，以提高其内在治疗活性并克服药代动力学问题。在本研究中，按照“多价高亲和力”结合策略，设计并合成了由接枝到GNPs表面的模型β-二酮酸（DKA）构成的新型纳米系统。与游离DKA配体相比，这些首个纳米级DKA原型对HIV-1整合酶（HIV-1 IN）催化活性的抑制作用有所改善。
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