Affinity of antimalarial drugs for stacked haematin linked on sepharose.
The affinity to haematin of antimalarial drugs and of some closely related compounds has been measured by the use of a polymeric haematin linked to an agarose gel. Haematin-drug interaction shows a low specificity and does not exhibit the sharp structure-activity relationship observed in the biological activities of the compounds. It is suggested that a chloroquine-haematin interaction does not explain the biological properties of this antimalarial, although it constitutes a necessary step in the concentration of the drug in the parasitized erythrocyte.
D000962:Antimalarials / Q000378:metabolism*; D004347:Drug Interactions; D006418:Heme / Q000031:analogs & derivatives*; D006427:Hemin / Q000378:metabolism*; D008854:Microscopy, Electron; D008958:Models, Molecular; D012685:Sepharose; D013329:Structure-Activity Relationship
D000962:Antimalarials; D006418:Heme; D006427:Hemin; D012685:Sepharose