Center for ViroScience and Cure, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Children's Healthcare of Atlanta, 1760 Haygood Drive, Atlanta, GA, 30322, USA.
Center for ViroScience and Cure, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Children's Healthcare of Atlanta, 1760 Haygood Drive, Atlanta, GA, 30322, USA.
Eur J Med Chem. 2022 Oct 5;240:114554. doi: 10.1016/j.ejmech.2022.114554. Epub 2022 Jun 20.
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.
在这场大流行持续了 40 多年后，HIV 仍然是全球的负担，目前还没有治愈的方法。幸运的是，已经开发出了高效抗逆转录病毒疗法（HAART）来管理和抑制 HIV 感染。针对关键病毒蛋白的两种或三种药物的组合，包括抑制 HIV 逆转录酶（RT）的化合物，已成为 HIV 治疗的基石。本文综述了核苷逆转录酶抑制剂（NRTIs），包括链终止剂、延迟链终止剂、核苷逆转录酶易位抑制剂（NRTTIs）和核苷酸竞争 RT 抑制剂（NcRTIs）；重点讨论了它们的历史、作用机制、耐药性以及当前的临床应用，包括长效方案。
