Peatey, Christopher L.;
Andrews, Katherine T.;
Eickel, Nina;
MacDonald, Timothy;
Butterworth, Alice S.;
Trenholme, Katharine R.;
Gardiner, Donald L.;
McCarthy, James S.;
Skinner-Adams, Tina S.
Antimalarial Asexual Stage-Specific and Gametocytocidal Activities of HIV Protease Inhibitors
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Media type:
E-Article
Title:
Antimalarial Asexual Stage-Specific and Gametocytocidal Activities of HIV Protease Inhibitors
Contributor:
Peatey, Christopher L.;
Andrews, Katherine T.;
Eickel, Nina;
MacDonald, Timothy;
Butterworth, Alice S.;
Trenholme, Katharine R.;
Gardiner, Donald L.;
McCarthy, James S.;
Skinner-Adams, Tina S.
imprint:
American Society for Microbiology, 2010
Published in:Antimicrobial Agents and Chemotherapy
Description:
<jats:title>ABSTRACT</jats:title>
<jats:p>
The stage-specific antimalarial activities of a panel of antiretroviral protease inhibitors (PIs), including two nonpeptidic PIs (tipranavir and darunavir), were tested
<jats:italic>in vitro</jats:italic>
against
<jats:italic>Plasmodium falciparum</jats:italic>
. While darunavir demonstrated limited antimalarial activity (effective concentration [EC
<jats:sub>50</jats:sub>
], >50 μM), tipranavir was active at clinically relevant concentrations (EC
<jats:sub>50</jats:sub>
, 12 to 21 μM). Saquinavir, lopinavir, and tipranavir preferentially inhibited the growth of mature asexual-stage parasites (24 h postinvasion). While all of the PIs tested inhibited gametocytogenesis, tipranavir was the only one to exhibit gametocytocidal activity.
</jats:p>