Substrate activity screening: a fragment-based method for the rapid identification of nonpeptidic protease inhibitors

WJL Wood, AW Patterson, H Tsuruoka…

Index: Wood, Warren J. L.; Patterson, Andrew W.; Tsuruoka, Hiroyuki; Jain, Rishi K.; Ellman, Jonathan A. Journal of the American Chemical Society, 2005 , vol. 127, # 44 p. 15521 - 15527

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Citation Number: 87

Abstract

A new fragment-based method for the rapid development of novel and distinct classes of nonpeptidic protease inhibitors, Substrate Activity Screening (SAS), is described. This method consists of three steps:(1) a library of N-acyl aminocoumarins with diverse, low molecular weight N-acyl groups is screened to identify protease substrates using a simple fluorescence-based assay,(2) the identified N-acyl aminocoumarin substrates are ...