Haematin (haem) polymerization and its inhibition by quinoline antimalarials

R. G. Ridley, A. Dorn, S. R. Vippagunta, J. L. Vennerstrom

Research output: Contribution to journalArticle

63 Scopus citations

Abstract

Haematin (ferriprotoporphyrin IX) is released from haemoglobin during its degradation in the malarial parasite's food vacuole and is detoxified by its polymerization into a form of β-haematin called haemozoin, or malarial pigment. This process is protein independent in vitro. Quinoline antimalarial blood schizonticides accumulate in the food vacuole and may inhibit haematin polymerization by binding to haematin and preventing its incorporation into the growing haemozoin chain. Drug resistance to quinolines is thought to be due to reduced accumulation of the drug in the food vacuole. As some quinolines can overcome this resistance, quinolines, as a class, remain a potential source future antimalarial drugs.

Original languageEnglish (US)
Pages (from-to)559-566
Number of pages8
JournalAnnals of Tropical Medicine and Parasitology
Volume91
Issue number5
DOIs
StatePublished - 1997

ASJC Scopus subject areas

  • Parasitology
  • Infectious Diseases

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