Conformational changes in HIV-1 reverse transcriptase induced by nonnucleoside reverse transcriptase inhibitor binding

Nicolas Sluis-Cremer, N. Alpay Temiz, Ivet Bahar

Research output: Contribution to journalReview articlepeer-review

132 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)323-332
Number of pages10
JournalCurrent HIV research
Volume2
Issue number4
DOIs
StatePublished - Oct 2004

Keywords

  • DNA polymerase
  • HIV-1 reverse transcriptase
  • Nonnucleoside reverse transcriptase inhibitor
  • Ribonuclease H

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