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Selectively Binding a Bromodomain
Dirk Trauner,Martin Reynders +1 more
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This article is published in Synfacts.The article was published on 2020-07-01. It has received 0 citations till now. The article focuses on the topics: Bromodomain.read more
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Journal ArticleDOI
Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation
Omer Gilan,Omer Gilan,Inmaculada Rioja,Kathy Knezevic,Matthew J Bell,Miriam M. Yeung,Nicola Harker,Enid Y.N. Lam,Enid Y.N. Lam,Chun-wa Chung,Paul Bamborough,Massimo Petretich,Marjeta Urh,Stephen John Atkinson,Anna K. Bassil,Emma J. Roberts,Dane Vassiliadis,Dane Vassiliadis,Marian L. Burr,Marian L. Burr,Alex Preston,Christopher Roland Wellaway,Thilo Werner,James Gray,Anne Marie Michon,Thomas Gobbetti,Vinod Kumar,Peter Ernest Soden,Andrea C. Haynes,Johanna Vappiani,David F. Tough,Simon Taylor,Sarah-Jane Dawson,Sarah-Jane Dawson,Marcus Bantscheff,Matthew J Lindon,Gerard Drewes,Emmanuel Hubert Demont,Danette L. Daniels,Paola Grandi,Rab K. Prinjha,Mark A. Dawson,Mark A. Dawson +42 more
TL;DR: It is found that steady-state gene expression primarily requires BD1, whereas the rapid increase of gene expression induced by inflammatory stimuli requires both BD1 and BD2 of all BET proteins, which may guide future BET-targeted therapies.
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