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

Lucie Guetzoyan | Zendy; Richard J. Ingham | Zendy; Nikzad Nikbin | Zendy; Julien Rossignol | Zendy; Michael Wolling | Zendy; Mark Baumert | Zendy; N. Burgess-Brown | Zendy; Claire StrainDamerell | Zendy; Leela Shrestha | Zendy; Paul E. Brennan | Zendy; O. Fedorov | Zendy; Stefan Knapp | Zendy; Steven V. Ley | Zendy

Open Access

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

Author(s) -

Lucie Guetzoyan,

Richard J. Ingham,

Nikzad Nikbin,

Julien Rossignol,

Michael Wolling,

Mark Baumert,

N. Burgess-Brown,

Claire StrainDamerell,

Leela Shrestha,

Paul E. Brennan,

O. Fedorov,

Stefan Knapp,

Steven V. Ley

Publication year - 2014

Publication title -

medchemcomm

Language(s) - English

Resource type - Journals

eISSN - 2040-2511

pISSN - 2040-2503

DOI - 10.1039/c4md00007b

Subject(s) - chemistry , flow chemistry , combinatorial chemistry , chromatography , organic chemistry , catalysis

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.EPSRC/EP/F069685/1NovartisBP Endowmen

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