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- W1974106435 abstract "A combinatorial library of norstatine-type peptide isosters as putative inhibitors of aspartic proteases is presented. The library was synthesized using a split-and-mix strategy designed to afford a one-bead-two-compounds library with the isosteric elements positioned centrally in peptide chains. Application of ladder synthesis during library generation enabled structure identification by MALDI-TOF mass spectroscopy. The library was screened against aspartic protease renin, and two types of inhibitors were identified, that is, XXX-psi[CHRCHOH)-XXX and an aldehyde arising from unreacted starting material. Selected hits were resynthesized and assayed in solution, revealing inhibitors of nanomolar potency." @default.
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- W1974106435 date "2003-01-14" @default.
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- W1974106435 title "Solid-Phase Combinatorial Library of Norstatine-Type Isosters by the Nitroaldol Reaction" @default.
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- W1974106435 doi "https://doi.org/10.1021/cc0100722" @default.
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