Selection of human immunodeficiency virus type 1 resistance against the pyranodipyrimidine V-165 points to a multimodal mechanism of action.

  title={Selection of human immunodeficiency virus type 1 resistance against the pyranodipyrimidine V-165 points to a multimodal mechanism of action.},
  author={A. Hombrouck and A. Hantson and B. Van Remoortel and M. Michiels and J. Vercammen and D. Rhodes and V. Tetz and Y. Engelborghs and F. Christ and Z. Debyser and M. Witvrouw},
  journal={The Journal of antimicrobial chemotherapy},
  volume={59 6},
  • A. Hombrouck, A. Hantson, +8 authors M. Witvrouw
  • Published 2007
  • Biology, Medicine
  • The Journal of antimicrobial chemotherapy
  • OBJECTIVES We have previously identified the pyranodipyrimidines (PDPs) as a new class of integrase (IN) inhibitors. The most potent congener V-165 inhibits HIV-1 integration at low micromolar concentrations by inhibiting the binding of IN to the DNA. As part of pre-clinical studies with PDP, we wanted to investigate HIV resistance development against V-165 and to further characterize the physicochemical properties of the compound. METHODS We selected PDP-resistant HIV-1 strains by growing… CONTINUE READING
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