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Artemisinin-Based Antimalarial Drug Therapy: Molecular Pharmacology and Evolving Resistance

Departments of Chemistry and of Biochemistry and Cellular and Molecular Biology, Georgetown University, 37th and O Streets NW, Washington, DC 20057, USA
Author to whom correspondence should be addressed.
Trop. Med. Infect. Dis. 2019, 4(2), 89;
Received: 18 April 2019 / Revised: 21 May 2019 / Accepted: 24 May 2019 / Published: 4 June 2019
(This article belongs to the Special Issue Drug Discovery and Development for Tropical Diseases)
The molecular pharmacology of artemisinin (ART)-based antimalarial drugs is incompletely understood. Clinically, these drugs are used in combination with longer lasting partner drugs in several different artemisinin combination therapies (ACTs). ACTs are currently the standard of care against Plasmodium falciparum malaria across much of the world. A harbinger of emerging artemisinin resistance (ARTR), known as the delayed clearance phenotype (DCP), has been well documented in South East Asia (SEA) and is beginning to affect the efficacy of some ACTs. Though several genetic mutations have been associated with ARTR/DCP, a molecular mechanism remains elusive. This paper summarizes our current understanding of ART molecular pharmacology and hypotheses for ARTR/DCP. View Full-Text
Keywords: heme adduct; PfPI3KIII; artemisinin target heme adduct; PfPI3KIII; artemisinin target
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Heller, L.E.; Roepe, P.D. Artemisinin-Based Antimalarial Drug Therapy: Molecular Pharmacology and Evolving Resistance. Trop. Med. Infect. Dis. 2019, 4, 89.

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