Selective targeting of the HIV-1 reverse transcriptase catalytic complex through interaction with the "primer grip" region by pyrrolobenzoxazepinone non-nucleoside inhibitors correlates with increased activity towards drug-resistant mutants.

@article{Zanoli2008SelectiveTO,
  title={Selective targeting of the HIV-1 reverse transcriptase catalytic complex through interaction with the "primer grip" region by pyrrolobenzoxazepinone non-nucleoside inhibitors correlates with increased activity towards drug-resistant mutants.},
  author={Samantha Zanoli and Sandra Gemma and Stefania Butini and Margherita Brindisi and Bhupendra P Joshi and Giuseppe Campiani and Caterina Fattorusso and Marco Persico and Emmanuele Crespan and Reynel Cancio and Silvio Spadari and Ulrich H{\"u}bscher and Giovanni Maga},
  journal={Biochemical pharmacology},
  year={2008},
  volume={76 2},
  pages={156-68}
}
PBO (pyrrolobenzoxazepinone) derivatives are non-nucleoside reverse transcriptase inhibitors (NNRTIs), which display a selective interaction with the catalytic ternary complex of HIV-1 reverse transcriptase (RT) and its substrates. In order to develop novel PBOs with improved resistance profiles, we synthesised additional PBO derivatives, specifically designed to target highly conserved residues in the beta12-beta13 hairpin, the so-called "primer grip" region of HIV-1 RT. Here, we investigated… CONTINUE READING

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Next-generation HIV-1 non-nucleoside reverse transcriptase inhibitors.

Current opinion in investigational drugs • 2006
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