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Pentacycloundecane-based inhibitors of wild-type C-South African HIV-protease
Faculty
Pharmacy
Year:
2011
Type of Publication:
Article
Pages:
2274-2277
Authors:
Soliman, Mahmoud E. S, Sayed, Yasien, Govender, Thavendran, Kruger, Hendrik G, Maguire, Glenn E. M, Makatini, Maya M, Petzold, Katja, Arvidsson, Per I, Honarparvar, Bahareh, Govender, Patrick, Sriharsha, Shimoga N
DOI:
10.1016/j.bmcl.2011.02.105
Journal:
BIOORGANIC \& MEDICINAL CHEMISTRY LETTERS PERGAMON-ELSEVIER SCIENCE LTD
Volume:
21
Research Area:
Pharmacology \& Pharmacy; Chemistry
ISSN
ISI:000289074700020
Keywords :
Pentacycloundecane peptides, HIV-protease inhibitor, EASY-ROESY, Inhibitory concentration (IC50), Molecular docking
Abstract:
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 IC50 activity against the resistance-prone wild type C-South African HIV-protease (C-SA) catalytic site via a norstatine type functional group of the PCU hydroxy lactam. NMR was employed to determine a logical correlation between the inhibitory concentration (IC50) results and the 3D structure of the corresponding inhibitors in solution. NMR investigations indicated that the activity is related to the chirality of the PCU moiety and its ability to induce conformations of the coupled peptide side chain. The results from docking experiments coincided with the experimental observed activities. These findings open up useful applications for this family of cage peptide inhibitors, considering the vast number of alternative disease related proteases that exist. (C) 2011 Elsevier Ltd. All rights reserved.
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