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
Other Authors: Major, Louise L., author (author), Denton, Helen, author, Smith, Terry K., author
Format: eSerial
Language:Inglés
Published: Rijeka (HR) : InTech 2013.
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See on Biblioteca Universitat Ramon Llull:https://discovery.url.edu/permalink/34CSUC_URL/1im36ta/alma991009820258006719
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.
Published:Began with: 2013-
Physical Description:1 online resource
Publication Frequency:annual