Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library |
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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 |
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Affiliation: | Department of Biology, Pharmacopeia, Inc., Princeton, NJ 08540, USA. |
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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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