Giancarlo A. Biagini

Hanafy M. Ismail

Hunt

Janet Hemingway

Matthew Phanchana

Meshnick

Michael H. L. Wong

Paul M. O’Neill

Sitthivut Charoensutthivarakul

Speers

Stephen A. Ward

Victoria Barton

Xiao

Significance
          The mechanism of action of the artemisinin (ART) class of antimalarial drugs, the most important antimalarial drug class in use today, remains controversial, despite more than three decades of intensive research. We have developed an unbiased chemical proteomic approach using a suite of ART activity-based protein profiling probes to identify proteins within the malaria parasite that are alkylated by ART, including proteins involved in glycolysis, hemoglobin metabolism, and redox defense. The data point to a pleiotropic mechanism of drug action for this class and offer a strategy for investigating resistance mechanisms to ART-based drugs as well as mechanisms of action of other endoperoxide-based drugs.</jats:p

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Proceedings of the National Academy of Sciences

Artemisinin activity-based probes identify multiple molecular targets within the asexual stage of the malaria parasites
            <i>Plasmodium falciparum</i>
            3D7

Artemisinin activity-based probes identify multiple molecular targets within the asexual stage of the malaria parasites
                    Plasmodium falciparum

Artemisinin activity-based probes identify multiple molecular targets within the asexual stage of the malaria parasites Plasmodium falciparum

Abstract

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