Coupled enzyme activity and thermal shift screening of the Maybridge Rule of 3 Fragment Library against Trypanosoma brucei choline kinase, a genetically validated drug target

In this study the authors interrogate ~630 compounds of the Maybridge Rule of 3 Fragment Library for compounds that interact with, and inhibit TbCK. The Maybridge Rule of 3 Fragment Library is a small collection of quantifiable diverse [35, 36], pharmacophoric rich, chemical entities. Comparisons be...

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Bibliographic Details
Main Authors: Major, Louise L., Denton, Helen (Author), Smith, Terry K. (Author)
Format: eBook
Language:English
Published: Rijeka (HR) InTech 2013 Jan 23, 2013
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Collection: National Center for Biotechnology Information - Collection details see MPG.ReNa
Description
Summary:In this study the authors interrogate ~630 compounds of the Maybridge Rule of 3 Fragment Library for compounds that interact with, and inhibit TbCK. The Maybridge Rule of 3 Fragment Library is a small collection of quantifiable diverse [35, 36], pharmacophoric rich, chemical entities. Comparisons between two different screening methods, a coupled enzyme activity assay and differential scanning fluorimetry, has allowed identification of compounds that interact and inhibit the T. brucei choline kinase, several of which possess selective trypanocidal activity
Item Description:Chapter 14 of the book: Drug discovery / edited by Hany A. El-Shemy. Rijeka, Croatia : InTech, 2013
Physical Description:1 online resource illustrations