Chloroquine as intercalator: a hypothesis revived
作者： S.R. Meshnick
DOI: 10.1016/0169-4758(90)90215-P
关键词: Mechanism of action 、 Pharmacology 、 Lysosome 、 DNA 、 Chloroquine 、 Mode of action 、 Drug 、 Biology 、 DNA Intercalation 、 Intercalation (chemistry) 、 Biochemistry
摘要: The mode of action chloroquine is still controversial. Proposed mechanisms include (1) DNA intercalation, (2) lysosome accumulation and (3) binding to ferriprotoporphyrin IX. Recent data suggest that intercalation into parasite can occur at physiological concentrations the drug. Furthermore, structure-activity relationship studies are most consistent with mechanism. Regardless which mechanism correct, selective toxicity for malaria parasites probably due permease-mediated uptake.
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