Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library

Bioorg Med Chem Lett. 1998 Sep 8;8(17):2315-20. doi: 10.1016/s0960-894x(98)00419-3.

Abstract

An encoded 13,020-member combinatorial library was synthesized containing a statine core. Evaluation of this library with plasmepsin II, an aspartyl protease required for hemoglobin metabolism in the malaria parasite, led to the identification of potent and selective inhibitors as well as novel structure-activity relationships.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acids*
  • Animals
  • Antimalarials / chemical synthesis*
  • Antimalarials / chemistry
  • Antimalarials / pharmacology
  • Aspartic Acid Endopeptidases / antagonists & inhibitors*
  • Cloning, Molecular
  • Databases as Topic*
  • Drug Design
  • Hemoglobins / metabolism
  • Humans
  • Molecular Structure
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / chemistry
  • Oligopeptides / metabolism
  • Oligopeptides / pharmacology
  • Peptide Library
  • Plasmodium falciparum / enzymology*
  • Protease Inhibitors / chemical synthesis*
  • Protease Inhibitors / chemistry
  • Protease Inhibitors / pharmacology
  • Protozoan Proteins
  • Recombinant Proteins / antagonists & inhibitors
  • Structure-Activity Relationship
  • Substrate Specificity

Substances

  • Amino Acids
  • Antimalarials
  • Hemoglobins
  • Oligopeptides
  • Peptide Library
  • Protease Inhibitors
  • Protozoan Proteins
  • Recombinant Proteins
  • Aspartic Acid Endopeptidases
  • plasmepsin II
  • statine