Receptor-drug association studies in the inhibition of the hematin aggregation process of malaria

FEBS Lett. 2003 Jul 17;547(1-3):217-22. doi: 10.1016/s0014-5793(03)00692-6.

Abstract

Docking studies were performed to investigate the binding of several antimalarial compounds to the putative drug receptors involved in the hematin aggregation process. These studies reveal a binding profile that correlates with the complementarity of electrostatic potentials between the receptors and the active molecules. These results allow a possible explanation for the same molecular mechanism shown by 4-aminoquinolines, quinine, mefloquine, halofantrine and hydroxylated xanthones. The docking data presented in this work offer an interesting approach to the design of new molecules with potential antimalarial activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimalarials / chemistry*
  • Antimalarials / pharmacology*
  • Hemin / chemistry*
  • Humans
  • Malaria / drug therapy*
  • Malaria / physiopathology*
  • Models, Molecular
  • Molecular Conformation
  • Protein Conformation
  • Receptors, Drug / chemistry
  • Receptors, Drug / metabolism*
  • Static Electricity
  • Structure-Activity Relationship

Substances

  • Antimalarials
  • Receptors, Drug
  • Hemin