Article
Small-molecule dimerization inhibitors of wild-type and mutant HIV protease: a focused library approach.
Journal of the American Chemical Society - 18 Aug 2004
Shultz Michael D, Ham Young-Wan, Lee Song-Gil, Davis David A, Brown Cara, Chmielewski Jean
Abstract excerpt
We demonstrate that a focused library based on truncated, cross-linked interfacial peptides of HIV-1 protease produces effective dimerization inhibitors of the enzyme. By combining individual changes of the library into a single compound, we obtained a significantly more potent agent and found that an additive increase in inhibitor efficacy was obtained. The good activity of library members against an active-site...
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