NMR-based discovery of lead inhibitors that block DNA binding of the human papillomavirus E2 protein.

@article{Hajduk1997NMRbasedDO,
  title={NMR-based discovery of lead inhibitors that block DNA binding of the human papillomavirus E2 protein.},
  author={Philip J. Hajduk and Jurgen Dinges and G F Miknis and M Merlock and Tim R Middleton and Dale J. Kempf and David Egan and Karl A. Walter and Terry S. Robins and Suzanne Beckham Shuker and Thomas F. Holzman and Stephen W. Fesik},
  journal={Journal of medicinal chemistry},
  year={1997},
  volume={40 20},
  pages={3144-50}
}
The E2 protein is required for the replication of human papillomaviruses (HPVs), which are responsible for anogenital warts and cervical carcinomas. Using an NMR-based screen, we tested compounds for binding to the DNA-binding domain of the HPV-E2 protein. Three classes of compounds were identified which bound to two distinct sites on the protein. Biphenyl and biphenyl ether compounds containing a carboxylic acid bind to a site near the DNA recognition helix and inhibit the binding of E2 to DNA… CONTINUE READING