Premium
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
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.201309436
Subject(s) - chemistry , combinatorial chemistry , ligand (biochemistry) , function (biology) , shiga toxin , toxin , computational biology , nanotechnology , stereochemistry , escherichia coli , biochemistry , materials science , biology , receptor , genetics , gene
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.