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Issue 4, 2014
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Machine-assisted synthesis of modulators of the histone reader BRD9 using flow methods of chemistry and frontal affinity chromatography

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Abstract

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.

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

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Publication details

The article was received on 06 Jan 2014, accepted on 06 Mar 2014 and first published on 07 Mar 2014


Article type: Concise Article
DOI: 10.1039/C4MD00007B
Author version available: Download Author version (PDF)
Citation: Med. Chem. Commun., 2014,5, 540-546
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    Machine-assisted synthesis of modulators of the histone reader BRD9 using flow methods of chemistry and frontal affinity chromatography

    L. Guetzoyan, R. J. Ingham, N. Nikbin, J. Rossignol, M. Wolling, M. Baumert, N. A. Burgess-Brown, C. M. Strain-Damerell, L. Shrestha, P. E. Brennan, O. Fedorov, S. Knapp and S. V. Ley, Med. Chem. Commun., 2014, 5, 540
    DOI: 10.1039/C4MD00007B

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