Conformational Changes in HIV-1 Reverse Transcriptase Induced by Nonnucleoside Reverse Transcriptase Inhibitor Binding

Author(s): Nicolas Sluis-Cremer, N. Alpay Temiz, Ivet Bahar.

Journal Name: Current HIV Research

Volume 2 , Issue 4 , 2004

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Nonnucleoside reverse transcriptase inhibitors (NNRTI) are a group of small hydrophobic compounds with diverse structures that specifically inhibit HIV-1 reverse transcriptase (RT). NNRTIs interact with HIV-1 RT by binding to a single site on the p66 subunit of the p66 / p51 heterodimeric enzyme, termed the NNRTI-binding pocket (NNRTI-BP). This binding interaction results in both short-range and long-range distortions of RT structure. In this article, we review the structural, computational and experimental evidence of the NNRTI-induced conformational changes in HIV-1 RT and relate them to the mechanism by which these compounds inhibit HIV-1 reverse transcription.

Keywords: hiv-1 reverse transcriptase, nonnucleoside reverse transcriptase inhibitor, dna polymerase, ribonuclease h

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Article Details

Year: 2004
Page: [323 - 332]
Pages: 10
DOI: 10.2174/1570162043351093
Price: $58

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