Literature DB >> 24453091

Discovery of inhibitors of Shiga toxin type 2 by on-plate generation and screening of a focused compound library.

Somnath Dasgupta1, Pavel I Kitov, Joanna M Sadowska, David R Bundle.   

Abstract

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.
Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  Shiga toxins; drug discovery; glycoarrays; haemolytic uremic syndrome; inhibitors

Mesh：

Substances：

Year:  2014        PMID： 24453091     DOI： 10.1002/anie.201309436

Source DB:  PubMed          Journal:  Angew Chem Int Ed Engl        ISSN： 1433-7851            Impact factor:   15.336


  3 in total

1.  The crystal structure of shiga toxin type 2 with bound disaccharide guides the design of a heterobifunctional toxin inhibitor.

Authors:  Jared M Jacobson; Jiang Yin; Pavel I Kitov; George Mulvey; Tom P Griener; Michael N G James; Glen Armstrong; David R Bundle
Journal:  J Biol Chem       Date:  2013-11-13       Impact factor: 5.157

2.  Mechanism of inhibition of Shiga-toxigenic Escherichia coli SubAB cytotoxicity by steroids and diacylglycerol analogues.

Authors:  Kinnosuke Yahiro; Sayaka Nagasawa; Kimitoshi Ichimura; Hiroki Takeuchi; Kohei Ogura; Hiroyasu Tsutsuki; Takeshi Shimizu; Sunao Iyoda; Makoto Ohnishi; Hirotaro Iwase; Joel Moss; Masatoshi Noda
Journal:  Cell Death Discov       Date:  2018-02-14

3.  Scalable Reporter Assays to Analyze the Regulation of stx2 Expression in Shiga Toxin-Producing Enteropathogens.

Authors:  Martin B Koeppel; Jana Glaser; Tobias Baumgartner; Stefanie Spriewald; Roman G Gerlach; Benedikt von Armansperg; John M Leong; Bärbel Stecher
Journal:  Toxins (Basel)       Date:  2021-07-29       Impact factor: 4.546
  3 in total

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