Tatiana V Ilina

TL;DR: Sub substituted DHBNH derivatives that interact with the NNRTI-binding pocket inhibit both the polymerase and RNH activities of RT and inhibit the initiation of RNA-primed DNA synthesis.

TL;DR: The first AZT-derived 1,2,3-triazoles with submicromolar potencies against HIV-1 are reported, confirming a mechanism of preferred translocation of triazoles into the P-site of HIV reverse transcriptase (RT).

TL;DR: In this paper, the authors describe the current clinically used RT inhibitors, outlining mechanisms of action as well as factors in HIV resistance to these drugs, and some promising new pipeline RT inhibitors are discussed, including compounds directed at novel RT targets not addressed by current RT therapeutics.

TL;DR: This review focuses mainly on the most potent low micromolar potency compounds, as these provide logical bases for further development and discuss why HIV RNase H has been a difficult target for antiretroviral drug development.

TL;DR: NMR studies of the interaction of a new ribonuclease H inhibitor, BHMP07, with a catalytically active HIV‐1 reverse transcriptase ribonUClease H domain fragment are described, providing a structural characterization of the ribonuclease H inhibitor interaction and are likely to be useful for further improvements of the inhibitors.