Inhibition Mechanism of Antimalarial Drugs Targeting the Cytochrome bc₁ Complex

Mechanism of endosomal TLR inhibition by antimalarial drugs and imidazoquinolines.

Endosomal TLRs play an important role in innate immune response as well as in autoimmune processes. In the therapy of systemic lupus erythematosus, antimalarial drugs chloroquine, hydroxychloroquine, and quinacrine have been used for a long time. Their suppression of endosomal TLR activation has been attributed to the inhibition of endosomal acidification, which is a prerequisite for the activa...

Inhibition of Heme Polymerization, the Mechanism of Antimalarial Activity in Phlomis caucasica Rech.f. (Lamiaceae)

Background: Malaria is one of the most important parasitic diseases in the world caused by Plasmodium species. The malaria parasite digests hemoglobin in vacuole to amino acids and heme. Plasmodium has got several detoxification mechanisms to protect itself from toxic heme. The most important mechanism is heme polymerization. Identifying compounds that inhibit heme polymerization is an approach...

The History of Antimalarial Drugs

Complex dynamics and stability of resistance to antimalarial drugs.

A succession of antimalarial drugs has been deployed to treat human falciparum malaria but each has, in turn, been nullified by the spread of drug resistance. The consensus view has always been that, once present, resistance will inevitably rapidly increase to 100%. However, recent field evidence has shown this is not inevitable, and that drug resistance may initially spread and then stabilize ...

The use of antimalarial drugs.

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