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

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

Volume: 2 Issue: 4

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Sluis-Cremer Nicolas, Temiz Alpay N. and Bahar Ivet, Conformational Changes in HIV-1 Reverse Transcriptase Induced by Nonnucleoside Reverse Transcriptase Inhibitor Binding, Current HIV Research 2004; 2 (4) . https://dx.doi.org/10.2174/1570162043351093