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Discovery of Inhibitors of Shiga Toxin Type 2 by On‐Plate Generation and Screening of a Focused Compound Library
Author(s) -
Dasgupta Somnath,
Kitov Pavel I.,
Sadowska Joanna M.,
Bundle David R.
Publication year - 2014
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201309436
Subject(s) - microtiter plate , toxin , combinatorial chemistry , function (biology) , plate reader , masking (illustration) , chemistry , ligand (biochemistry) , computational biology , nanotechnology , biochemistry , materials science , chromatography , biology , fluorescence , optics , physics , receptor , genetics , art , visual arts
A new microtiter‐plate‐based method for the rapid generation and evaluation of focused compound libraries was developed and applied to screening ligand analogues for the E. coli Shiga‐like toxin Stx2a. The method is general, it mitigates the masking of intrinsic affinity gains by multivalency and enables the discovery of potential hits when starting from ligands that exhibit extremely low affinity with proteins that depend on multivalency for their function.