The Optimisation of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode.

Simon C. C. Lucas,Stephen John Atkinson,Paul Bamborough,Heather Anne Barnett,Chun-wa Chung,Laurie J. Gordon,Darren Jason Mitchell,Alexander N. Phillipou,Rab K. Prinjha,Robert John Sheppard,Nicholas C. O. Tomkinson,Robert J. Watson,Emmanuel Hubert Demont

The Optimisation of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode.

2020

Simon C. C. Lucas
Stephen John Atkinson
Paul Bamborough
Heather Anne Barnett
Chun-wa Chung
Laurie J. Gordon
Darren Jason Mitchell
Alexander N. Phillipou
Rab K. Prinjha
Robert John Sheppard
Nicholas C. O. Tomkinson
Robert J. Watson
Emmanuel Hubert Demont

Most bromodomain inhibitors mimic the interactions of the natural acetylated lysine (KAc) histone substrate through key interactions with conserved asparagine and tyrosine residues within the bindi...

Keywords:

Biochemistry
Asparagine
Tyrosine
Histone
Substrate (chemistry)
Lysine
Bromodomain
Chemistry
Acetylation

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