Machine-assisted synthesis of modulators of the histone reader BRD9 using flow methods of chemistry and frontal affinity chromatography

A combination of conventional organic synthesis, remotely monitored flow synthesis and bioassay platforms, were used for the evaluation of novel inhibitors targeting bromodomains outside the well-studied bromodomain and extra terminal (BET) family, here exemplified by activity measurements on the br...

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Bibliographic Details
Published in:MedChemComm 2014, Vol.5 (4), p.540-546
Main Authors: Guetzoyan, Lucie, Ingham, Richard J., Nikbin, Nikzad, Rossignol, Julien, Wolling, Michael, Baumert, Mark, Burgess-Brown, Nicola A., Strain-Damerell, Claire M., Shrestha, Leela, Brennan, Paul E., Fedorov, Oleg, Knapp, Stefan, Ley, Steven V.
Format: Article
Language:English
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Summary:A combination of conventional organic synthesis, remotely monitored flow synthesis and bioassay platforms, were used for the evaluation of novel inhibitors targeting bromodomains outside the well-studied bromodomain and extra terminal (BET) family, here exemplified by activity measurements on the bromodomain of BRD9 protein, a component of some tissue-specific SWi/SNF chromatin remodelling complexes. The Frontal Affinity Chromatography combined with Mass Spectrometry (FAC-MS) method proved to be reliable and results correlated well with an independent thermal shift assay.
ISSN:2040-2503
2040-2511
DOI:10.1039/C4MD00007B