Program in Molecular Biophysics and Structural Biology, Hillman Cancer Center, University of Pittsburgh, 5117 Centre Ave., Pittsburgh, PA 15213, USA.
Department of Medicine, Division of Infectious Diseases, 3550 Terrace St., Pittsburgh, PA 15261, USA.
Biomolecules. 2013 Nov 1;3(4):889-904. doi: 10.3390/biom3040889.
HIV-1 reverse transcriptase (RT) plays a central role in HIV infection. Current United States Federal Drug Administration (USFDA)-approved antiretroviral therapies can include one of five approved non-nucleoside RT inhibitors (NNRTIs), which are potent inhibitors of RT activity. Despite their crucial clinical role in treating and preventing HIV-1 infection, their mechanism of action remains elusive. In this review, we introduce RT and highlight major advances from experimental and computational biophysical experiments toward an understanding of RT function and the inhibitory mechanism(s) of NNRTIs.
HIV-1 逆转录酶（RT）在 HIV 感染中起着核心作用。目前，美国食品和药物管理局（USFDA）批准的抗逆转录病毒疗法可以包括五种批准的非核苷类逆转录酶抑制剂（NNRTIs）之一，它们是 RT 活性的有效抑制剂。尽管它们在治疗和预防 HIV-1 感染方面具有至关重要的临床作用，但它们的作用机制仍不清楚。在这篇综述中，我们介绍了 RT，并强调了实验和计算生物物理实验方面的主要进展，以了解 RT 的功能和 NNRTIs 的抑制机制。
