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Plasmepsin inhibitors: design, synthesis, inhibitory studies and crystal structure analysis

Kesavulu, MM and Gowda, Prakasha AS and Ramya, TNC and Surolia, N and Suguna, K (2005) Plasmepsin inhibitors: design, synthesis, inhibitory studies and crystal structure analysis. In: Journal of Peptide Research, 66 (4). pp. 211-219.

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Abstract

Plasmepsin group of enzymes are key enzymes in the life cycle of malarial parasites. As inhibition of plasmepsins leads to the parasite's death, these enzymes can be utilized as potential drug targets. Although many drugs are available, it has been observed that Plasmodium falciparum, the species that causes most of the malarial infections and subsequent death, has developed resistance against most of the drugs. Based on the cleavage sites of hemglobin, the substrate for plasmepsins, we have designed two compounds(p-nitrobenzoyl-leucine-beta-alanine andp-nitrobenzoyl-leucine-isonipecotic acid), synthesized them, solved their crystal structures and studied their inhibitory effect using experimental and theoretical (docking) methods. In this paper, we discuss the synthesis, crystal structures and inhibitory nature of these two compounds which have a potential to inhibit plasmepsins.

Item Type: Journal Article
Additional Information: Copyright for this article belongs to Blackwell Publishing.
Keywords: malaria;plasmepsins;Plasmodium falciparum;plasmepsin inhibition;aspartic protease
Department/Centre: Division of Biological Sciences > Molecular Biophysics Unit
Date Deposited: 27 Sep 2005
Last Modified: 19 Sep 2010 04:20
URI: http://eprints.iisc.ernet.in/id/eprint/3732

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