Effect of synthesized inhibitors on babesipain-1, a new cysteine protease from the bovine piroplasm Babesia bigemina.
Papain-like cysteine proteases (CP) have been shown to have essential roles in parasitic protozoa and are under study as promising drug targets. One gene was identified by sequence similarity search to be homologous to the CP family in the ongoing Babesia bigemina genome sequencing project database. The newly identified CP gene, called babesipain-1, was cloned and expressed as a fusion protein, and the effect of different inhibitors on proteolytic activity was tested. A series of new artemisinin-vinyl sulfone hybrid molecules were tested as inhibitors being effective on the range of 0.3-30 microm, depending on the core-containing molecule.
Unidade de Tecnologias de Proteínas e Anticorpos Monoclonais, Instituto de Higiene e Medicina Tropical, Lisboa, Portugal. adomingos@ihmt.unl.pt
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D000981:Antiprotozoal Agents / Q000494:pharmacology*; D001403:Babesia / Q000378:metabolism*; D057056:Cysteine Proteases / Q000145:classification*; D015853:Cysteine Proteinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015394:Molecular Structure; D015800:Protozoan Proteins / Q000235:genetics / Q000378:metabolism
D000981:Antiprotozoal Agents; D015853:Cysteine Proteinase Inhibitors; D015800:Protozoan Proteins; D057056:Cysteine Proteases