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

…, GF Miknis, M Merlock, T Middleton…

文献索引：Hajduk, Philip J.; Dinges, Juergen; Miknis, Gregory F.; Merlock, Megan; Middleton, Tim; Kempf, Dale J.; Egan, David A.; Walter, Karl A.; Robins, Terry S.; Shuker, Suzy B.; Holzman, Thomas F.; Fesik, Stephen W. Journal of Medicinal Chemistry, 1997 , vol. 40, # 20 p. 3144 - 3150

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被引用次数: 181

摘要

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 ...