Biomolecules 2013, 3(4), 889-904; https://doi.org/10.3390/biom3040889
Biophysical Insights into the Inhibitory Mechanism of Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors
1
Program in Molecular Biophysics and Structural Biology, Hillman Cancer Center, University of Pittsburgh, 5117 Centre Ave., Pittsburgh, PA 15213, USA
2
Department of Cell Biology, Hillman Cancer Center, University of Pittsburgh, 5117 Centre Ave., Pittsburgh, PA 15213, USA
3
Department of Medicine, Division of Infectious Diseases, 3550 Terrace St., Pittsburgh, PA 15261, USA
*
Author to whom correspondence should be addressed.
Received: 18 September 2013 / Revised: 22 October 2013 / Accepted: 22 October 2013 / Published: 1 November 2013
(This article belongs to the Special Issue Enzymes and Their Biotechnological Applications)
Abstract
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. View Full-TextKeywords:
HIV-1 reverse transcriptase; NNRTI; mechanism; biophysics; single-molecule
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Schauer, G.; Leuba, S.; Sluis-Cremer, N. Biophysical Insights into the Inhibitory Mechanism of Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors. Biomolecules 2013, 3, 889-904.
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