title: Antimalarial effects of human immunodeficiency virus type 1 protease inhibitors differ from those of the aspartic protease inhibitor pepstatin.
abstract: Human immunodeficiency virus type 1 protease inhibitors (HIVPIs) and pepstatin are aspartic protease inhibitors with antimalarial activity. In contrast to pepstatin, HIVPIs were not synergistic with a cysteine protease inhibitor or more active against parasites with the cysteine protease falcipain-2 knocked out than against wild-type parasites. As with pepstatin, HIVPIs were equally active against wild-type parasites and against parasites with the food vacuole plasmepsin aspartic proteases knocked out. The antimalarial mechanism of HIVPIs differs from that of pepstatin.
authors.affiliation: Department of Medicine, San Francisco General Hospital, University of California, San Francisco, 94110, USA. sparikh@medsfgh.ucsf.edu
authors.forename: Sunil
authors.initials: S
authors.lastname: Parikh
authors.forename: Jun
authors.initials: J
authors.lastname: Liu
authors.forename: Puran
authors.initials: P
authors.lastname: Sijwali
authors.forename: Jiri
authors.initials: J
authors.lastname: Gut
authors.forename: Daniel E
authors.initials: DE
authors.lastname: Goldberg
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Rosenthal
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D017320:HIV Protease Inhibitors / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D021261:Parasitic Sensitivity Tests; D010436:Pepstatins / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects / Q000201:enzymology / Q000235:genetics
chemical_list: D000962:Antimalarials; D017320:HIV Protease Inhibitors; D010436:Pepstatins; D016282:Aspartic Acid Endopeptidases; C031375:pepstatin