Some enniatins (ENs) reportedly exhibit antiretroviral activities in vivo. The potential inhibitory activities of cyclic hexadepsipeptides such as beauvericin (BEA) and ENs H, I and MK1688 were investigated in vitro against human immunodeficiency virus type-1 (HIV-1) integrase and Moloney murine leukemia virus reverse transcriptase. BEA, EN I and EN MK1688 exhibited strong inhibitory activities against HIV-1 integrase, whereas EN H showed relatively weak activity. None of the examined compounds showed anti-reverse transcriptase activity. BEA was the most effective inhibitor of the tested cyclic hexadepsipeptides in inhibiting HIV-1 integrase. These results indicate the potential of cyclic hexadepsipeptides as a new class of potent inhibitors of HIV-1 integrase.
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http://dx.doi.org/10.1038/ja.2009.102 | DOI Listing |
China CDC Wkly
January 2025
State Key Laboratory of Infectious Disease Prevention and Control, National Center for AIDS/STD Control and Prevention, Chinese Center for Disease Control and Prevention, Beijing, China.
Introduction: The widespread adoption of integrase strand transfer inhibitors (INSTIs) has led to the emergence of INSTI-associated drug-resistance mutations. This cross-sectional study conducted a comprehensive national survey to investigate the prevalence of pretreatment drug resistance (PDR) to INSTIs among newly diagnosed human immunodeficiency virus (HIV) individuals in China.
Methods: The study enrolled 10,654 individuals from 31 provincial-level administrative divisions between 2018 and 2023.
J Glob Antimicrob Resist
January 2025
Faculty of Medicine, Department of Microbiology, University of Tartu, Tartu, Estonia.
Objectives: We investigated the prevalence of drug resistance mutations (DRMs) in individuals newly diagnosed with HIV-1 in Estonia in 2020 and 2022, and in Ukrainian war refugees living with HIV who arrived in Estonia in 2022.
Methods: HIV-1 genomic RNA was sequenced in protease-reverse transcriptase and integrase regions. DRMs were determined separately by Stanford University CPR Tool and HIVdb Program.
Viruses
January 2025
Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, MD 21702, USA.
Second-generation integrase strand transfer inhibitors (INSTIs) are strongly recommended for people living with HIV-1 (PLWH). The emergence of resistance to second-generation INSTIs has been infrequent and has not yet been a major issue in high-income countries. However, the delayed rollouts of these INSTIs in low- to middle-income countries during the COVID-19 pandemic combined with increased transmission of drug-resistant mutants worldwide are leading to an increase in INSTI resistance.
View Article and Find Full Text PDFPharmaceuticals (Basel)
December 2024
Amity Institute of Biotechnology, Amity University Maharashtra, Mumbai 410206, Maharashtra, India.
: The global AIDS pandemic highlights the urgent need for novel antiretroviral therapies (ART). In our previous work, Zinc C295 was identified as a potent HIV-1 integrase strand transfer (ST) inhibitor. This study explores its potential to also inhibit 3'-processing (3'P), thereby establishing its dual-targeting capability.
View Article and Find Full Text PDFJ Antimicrob Chemother
January 2025
CH Tourcoing, Service Universitaire des Maladies Infectieuses, 59200 Tourcoing, France.
Introduction: The specificity of HIV-1 DNA genotypic resistance tests (GRTs) is hampered by the detection of the APOBEC-context drug resistance mutations (AC DRMs), usually harboured by replication-incompetent proviruses. We sought factors associated with defective sequences in the HIV-1 pol region. In addition, AC DRMs and their link with defective sequences were investigated.
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