Inhibition of Plasmodium falciparum Hsp90 Contributes to the Antimalarial
Activities of Aminoalcohol-carbazoles
Version 3 2017-06-17, 13:13
Version 2 2016-07-08, 14:01
Version 1 2016-06-28, 20:16
Posted on 2017-06-17 - 13:13
Malaria caused by the protozoan parasite Plasmodium
falciparum (Pf) remains a major public
health problem throughout the developing world. One molecular target
that should receive more attention is the molecular chaperone Hsp90.
It is essential and highly conserved in all eukaryotes, including
in protozoan parasites. We have identified an amino-alcohol carbazole
(N-CBZ) as a PfHsp90-selective inhibitor by virtually docking a large
set of antimalarial compounds, previously found in a phenotypic screen,
into a PfHsp90-specific pocket. By correlating the ability of 30 additional
N-CBZ derivatives to bind directly to PfHsp90 with their Pf-inhibitory activity, we found that these types of compounds are
more likely to inhibit Pf growth if they bind PfHsp90.
For plausible targets such as PfHsp90, our workflow may help identifying
the molecular target for compounds found by screening large chemical
libraries for a desired biological effect and, conversely, ensuring
biological effectiveness for compounds affecting a particular target.
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Wang, Tai; Mäser, Pascal; Picard, Didier (2016). Inhibition of Plasmodium falciparum Hsp90 Contributes to the Antimalarial
Activities of Aminoalcohol-carbazoles. ACS Publications. Collection. https://doi.org/10.1021/acs.jmedchem.6b00591
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AUTHORS (3)
TW
Tai Wang
PM
Pascal Mäser
DP
Didier Picard
KEYWORDS
chemical librariesN-CBZ derivativesPf growthPfHsp 90Aminoalcohol-carbazoles Malariaamino-alcohol carbazolePfHsp 90-specific pocketchaperone Hsp 90.phenotypic screenbind PfHsp 90.health problemPlasmodium falciparum Hsp 90 Contributesparasite Plasmodium falciparumantimalarial compoundsPfHsp 90-selective inhibitorAntimalarial Activities