A role for the protease falcipain 1 in host cell invasion by the human malaria parasite |
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Authors: | Greenbaum Doron C Baruch Amos Grainger Munira Bozdech Zbynek Medzihradszky Katlin F Engel Juan DeRisi Joseph Holder Anthony A Bogyo Matthew |
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Institution: | Department of Pharmaceutical Chemistry, Veterans Affairs Medical Center, University of California, San Francisco, CA 94143, USA. dgreenb@itsa.ucsf.edu |
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Abstract: | Cysteine proteases of Plasmodium falciparum are required for survival of the malaria parasite, yet their specific cellular functions remain unclear. We used a chemical proteomic screen with a small-molecule probe to characterize the predominant cysteine proteases throughout the parasite life cycle. Only one protease, falcipain 1, was active during the invasive merozoite stage. Falcipain 1-specific inhibitors, identified by screening of chemical libraries, blocked parasite invasion of host erythrocytes, yet had no effect on normal parasite processes such as hemoglobin degradation. These results demonstrate a specific role for falcipain 1 in host cell invasion and establish a potential new target for antimalarial therapeutics. |
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