MK-8591（4'-乙炔基-2-氟-2'-脱氧腺苷）在培养中对HIV-2分离株和耐药HIV-2突变体表现出强效活性。
MK-8591 (4'-Ethynyl-2-Fluoro-2'-Deoxyadenosine) Exhibits Potent Activity against HIV-2 Isolates and Drug-Resistant HIV-2 Mutants in Culture.
作者信息
Wu Vincent H, Smith Robert A, Masoum Sara, Raugi Dana N, Ba Selly, Seydi Moussa, Grobler Jay A, Gottlieb Geoffrey S
机构信息
Center for Emerging and Reemerging Infectious Diseases and Department of Medicine, Division of Allergy and Infectious Diseases, University of Washington, Seattle, Washington, USA.
Center for Emerging and Reemerging Infectious Diseases and Department of Medicine, Division of Allergy and Infectious Diseases, University of Washington, Seattle, Washington, USA
出版信息
Antimicrob Agents Chemother. 2017 Jul 25;61(8). doi: 10.1128/AAC.00744-17. Print 2017 Aug.
Abstract
There is a pressing need to identify more effective antiretroviral drugs for HIV-2 treatment. Here, we show that the investigational compound MK-8591 (4'-ethynyl-2-fluoro-2'-deoxyadenosine [EFdA]) is highly active against group A and B isolates of HIV-2; 50% effective concentrations [EC] for HIV-2 were, on average, 4.8-fold lower than those observed for HIV-1. MK-8591 also retains potent activity against multinucleoside-resistant HIV-2 mutants (EC ≤ 11 nM). These data suggest that MK-8591 may have antiviral activity in HIV-2-infected individuals.
摘要
迫切需要鉴定出更有效的抗逆转录病毒药物用于治疗HIV-2感染。在此，我们表明研究性化合物MK-8591（4'-乙炔基-2-氟-2'-脱氧腺苷[EFdA]）对HIV-2的A组和B组分离株具有高活性；HIV-2的50%有效浓度[EC]平均比HIV-1低4.8倍。MK-8591对多核苷耐药的HIV-2突变体也保持强效活性（EC≤11 nM）。这些数据表明MK-8591可能对HIV-2感染个体具有抗病毒活性。
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