Author
Keywords
Abstract

Assigning the correct protonation state to the catalytic residues is essential for a realistic modelling of an enzyme's active site. Plasmepsins are pharmaceutically relevant aspartic proteases involved in haemoglobin degradation by Plasmodium spp. In aspartic proteases, one of the two catalytic aspartates is protonated, while the other is negatively charged. Here, multiple explicit-water molecular dynamics simulations of plasmepsin II, uncomplexed and with a hydroxypropylamine peptidomimetic inhibitor, indicate that protonation of Asp214 favours a stable active site structure. Moreover, the protonation state of the catalytic aspartate has a strong influence on a linear chain of hydrogen bonds with the adjacent side chains.

Year of Publication
2007
Journal
FEBS Letters
Volume
581
Issue
21
Number of Pages
4120-4124
Date Published
2007 Aug 21
Type of Article
Research Article
ISSN Number
0014-5793
DOI
10.1016/j.febslet.2007.07.033
Alternate Journal
FEBS Lett.
PMID
17689534
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