Bioorganic & Medicinal Chemistry Letters 2000-12-04

Synthesis of a statistically exhaustive fluorescent peptide substrate library for profiling protease specificity.

J E Sheppeck, H Kar, L Gosink, J B Wheatley, E Gjerstad, S M Loftus, A R Zubiria, J W Janc

Index: Bioorg. Med. Chem. Lett. 10 , 2639, (2000)

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Abstract

A statistically exhaustive, 8800 compound tripeptidal amidomethylcoumarin library was synthesized as discreet compounds using solid-phase combinatorial chemistry. A subset of the compounds was purified by HPLC and tested in a high-throughput fluorometric assay against several known serine and cysteine proteases to demonstrate the utility of this library for profiling protease substrate specificity.