Literature DB >> 12877581

Effect of detergent on "promiscuous" inhibitors.

Ali J Ryan1, Norman M Gray, Peter N Lowe, Chun-wa Chung.   

Abstract

The term "promiscuous" inhibitors has been coined for compounds whose inhibition mechanism involves the interaction of aggregates of many compound molecules with the target protein, rather than the binding of individual molecules. This paper demonstrates that promiscuous inhibitors can be differentiated from classical 1:1 inhibitors by the judicious use of detergents, making it possible to configure assays that significantly reduce this undesirable mechanism of inhibition without compromising assay performance.

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Year:  2003        PMID: 12877581     DOI: 10.1021/jm0340896

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  58 in total

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Authors:  Julie A Zorn; Holger Wille; Dennis W Wolan; James A Wells
Journal:  J Am Chem Soc       Date:  2011-11-17       Impact factor: 15.419

Review 2.  Screening in a spirit haunted world.

Authors:  Brian K Shoichet
Journal:  Drug Discov Today       Date:  2006-07       Impact factor: 7.851

3.  A detergent-based assay for the detection of promiscuous inhibitors.

Authors:  Brian Y Feng; Brian K Shoichet
Journal:  Nat Protoc       Date:  2006       Impact factor: 13.491

4.  Divergent modes of enzyme inhibition in a homologous structure-activity series.

Authors:  Rafaela S Ferreira; Clifford Bryant; Kenny K H Ang; James H McKerrow; Brian K Shoichet; Adam R Renslo
Journal:  J Med Chem       Date:  2009-08-27       Impact factor: 7.446

5.  Stoichiometry and physical chemistry of promiscuous aggregate-based inhibitors.

Authors:  Kristin E D Coan; Brian K Shoichet
Journal:  J Am Chem Soc       Date:  2008-06-28       Impact factor: 15.419

6.  Oxime-based click chemistry in the development of 3-isoxazolecarboxylic acid containing inhibitors of Yersinia pestis protein tyrosine phosphatase, YopH.

Authors:  Medhanit Bahta; Terrence R Burke
Journal:  ChemMedChem       Date:  2011-06-10       Impact factor: 3.466

7.  Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease.

Authors:  Ajit Jadhav; Rafaela S Ferreira; Carleen Klumpp; Bryan T Mott; Christopher P Austin; James Inglese; Craig J Thomas; David J Maloney; Brian K Shoichet; Anton Simeonov
Journal:  J Med Chem       Date:  2010-01-14       Impact factor: 7.446

8.  Complementarity between a docking and a high-throughput screen in discovering new cruzain inhibitors.

Authors:  Rafaela S Ferreira; Anton Simeonov; Ajit Jadhav; Oliv Eidam; Bryan T Mott; Michael J Keiser; James H McKerrow; David J Maloney; John J Irwin; Brian K Shoichet
Journal:  J Med Chem       Date:  2010-07-08       Impact factor: 7.446

9.  Colloid formation by drugs in simulated intestinal fluid.

Authors:  Allison K Doak; Holger Wille; Stanley B Prusiner; Brian K Shoichet
Journal:  J Med Chem       Date:  2010-05-27       Impact factor: 7.446

10.  A survey of across-target bioactivity results of small molecules in PubChem.

Authors:  Lianyi Han; Yanli Wang; Stephen H Bryant
Journal:  Bioinformatics       Date:  2009-06-23       Impact factor: 6.937

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