title: Artemisinin antimalarials: mechanisms of action and resistance.
abstract: Artemisinin derivatives are an important new class of antimalarial agents. These compounds contain endoperoxide bridges which are essential for antimalarial activity. Artemisinin is believed to act via a two-step mechanism. Artemisinin is first activated by intraparasitic heme-iron which catalyzes the cleavage of this endoperoxide. A resulting free radical intermediate may then kill the parasite by alkylating and poisoning one or more essential malarial protein(s). No clinically relevant artemisinin-resistant human malaria has yet been reported. However, an artemisinin-resistant strain of murine malaria has been developed and may offer clues to the kinds of resistance that may someday develop in human malarias.
authors.affiliation: Department of Epidemiology, University of Michigan School of Public Health, Ann Arbor 48109, USA. Meshnick@umich.edu
authors.forename: S R
authors.initials: SR
authors.lastname: Meshnick
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000145:classification / Q000494:pharmacology* / Q000627:therapeutic use; D037621:Artemisinins; D004195:Disease Models, Animal; D004353:Drug Evaluation, Preclinical; D004351:Drug Resistance; D006801:Humans; D016778:Malaria, Falciparum / Q000188:drug therapy* / Q000469:parasitology; D051379:Mice; D010963:Plasmodium falciparum / Q000187:drug effects; D015800:Protozoan Proteins / Q000187:drug effects; D012717:Sesquiterpenes / Q000737:chemistry / Q000145:classification / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D000962:Antimalarials; D037621:Artemisinins; D015800:Protozoan Proteins; D012717:Sesquiterpenes; C031327:artemisinin