Functionalized hydroxyethylamine based peptide nanostructures as potential inhibitors of falcipain-3, an essential proteases of Plasmodium falciparum |
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Authors: | Brijesh Rathi Anil K Singh Ram Kishan Neelu Singh N Latha S Srinivasan Kailash C Pandey Hemandra K Tiwari Brajendra K Singh |
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Institution: | 1. Bio-organic Research Laboratory, Department of Chemistry, University of Delhi, Delhi 110007, India;2. Bioinformatics Infrastructure Facility, Sri Venkateswara College, University of Delhi, Dhaula Kuan, New Delhi 110021, India;3. National Institute of Malaria Research, Host-Parasite Interaction Biology Group, Lab. No. 219, Sector-8 Dwarka, New Delhi 110077, India |
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Abstract: | Self-assembled peptide based nanostructures gained enough popularity due to their easy biocompatibility and numerous potential applications. An excellent model of self-assembly of hydroxyethylamine based peptide nanostructures was synthesized and characterized by DLS and TEM. Spherical nano structures of I and III were observed with particle size ~50 and ~80 nm, respectively. Further, I and III were screened against anti-malarial target, falcipain-3 (FP3), a crucial cysteine protease involved as a major hemoglobinase of Plasmodium falciparum. Interestingly, compound III completely inhibited the activity of FP3. The effective concentration (1.5 μM) of III found to be more potent than I. This biochemical result was substantiated by molecular-docking studies indicating III to be best inhibitor of FP3. This is the first report showing that bis hydroxethylamine based peptide nanostructures could be very effective inhibitor of malarial cysteine proteases. |
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Keywords: | Hydroxyethylamine Molecular self-assembly Falcipain-3 Antimalarial chemotheraphy Hemoglobin hydrolysis |
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