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 article

125 Citations (Scopus)

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 1 2004

Fingerprint

Reverse Transcriptase Inhibitors
RNA-Directed DNA Polymerase
Reverse Transcription
HIV-1
Enzymes
Human immunodeficiency virus 1 reverse transcriptase

Keywords

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

Cite this

Conformational changes in HIV-1 reverse transcriptase induced by nonnucleoside reverse transcriptase inhibitor binding. / Sluis-Cremer, Nicolas; Temiz, N. Alpay; Bahar, Ivet.

In: Current HIV research, Vol. 2, No. 4, 01.10.2004, p. 323-332.

Research output: Contribution to journalReview article

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