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HIV nucleoside reverse transcriptase inhibitors
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2022-06-20 , DOI: 10.1016/j.ejmech.2022.114554
Franck Amblard 1 , Dharmeshkumar Patel 1 , Eleftherios Michailidis 1 , Steven J Coats 1 , Mahesh Kasthuri 1 , Nicolas Biteau 1 , Zahira Tber 1 , Maryam Ehteshami 1 , Raymond F Schinazi 1
Affiliation  

More than 40 years into the pandemic, HIV remains a global burden and as of now, there is no cure in sight. Fortunately, highly active antiretroviral therapy (HAART) has been developed to manage and suppress HIV infection. Combinations of two to three drugs targeting key viral proteins, including compounds inhibiting HIV reverse transcriptase (RT), have become the cornerstone of HIV treatment. This review discusses nucleoside reverse transcriptase inhibitors (NRTIs), including chain terminators, delayed chain terminators, nucleoside reverse transcriptase translocation inhibitors (NRTTIs), and nucleotide competing RT inhibitors (NcRTIs); focusing on their history, mechanism of action, resistance, and current clinical application, including long-acting regimens.



中文翻译:


HIV核苷逆转录酶抑制剂



艾滋病毒大流行已有 40 多年了,它仍然是一个全球性的负担,而且到目前为止,还没有治愈方法。幸运的是,高效抗逆转录病毒疗法 (HAART) 已被开发用于控制和抑制 HIV 感染。两到三种针对关键病毒蛋白的药物组合,包括抑制 HIV 逆转录酶 (RT) 的化合物,已成为 HIV 治疗的基石。本综述讨论了核苷逆转录酶抑制剂(NRTI),包括链终止剂、延迟链终止剂、核苷逆转录酶易位抑制剂(NRTTI)和核苷酸竞争性 RT 抑制剂(NcRTI);重点关注其历史、作用机制、耐药性和当前的临床应用,包括长效治疗方案。

更新日期:2022-06-20
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