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Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library
Authors:CD Carroll  H Patel  TO Johnson  T Guo  M Orlowski  ZM He  CL Cavallaro  J Guo  A Oksman  IY Gluzman  J Connelly  D Chelsky  DE Goldberg  RE Dolle
Affiliation:Department of Biology, Pharmacopeia, Inc., Princeton, NJ 08540, USA.
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.
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