Article
Pentacycloundecane-based inhibitors of wild-type C-South African HIV-protease.
Bioorganic & medicinal chemistry letters - 15 Apr 2011
Makatini Maya M, Petzold Katja, Sriharsha Shimoga N, Soliman Mahmoud E S, Honarparvar Bahareh, Arvidsson Per I, Sayed Yasien, Govender Patrick, Maguire Glenn E M, Kruger Hendrik G, Govender Thavendran
Abstract excerpt
In this study, we present the first account of pentacycloundecane (PCU) peptide based HIV-protease inhibitors. The inhibitor exhibiting the highest activity made use of a natural HIV-protease substrate peptide sequence, that is, attached to the cage (PCU-EAIS). This compound showed nanomolar IC(50) activity against the resistance-prone wild type C-South African HIV-protease (C-SA) catalytic site via a norstatine...
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