Volume 21, Issue 7, Pages (July 2014)

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Volume 21, Issue 7, Pages 804-806 (July 2014) Nonequivalent Response to Bromodomain-Targeting BET Inhibitors in Oligodendrocyte Cell Fate Decision  Cheng-Ming Chiang  Chemistry & Biology  Volume 21, Issue 7, Pages 804-806 (July 2014) DOI: 10.1016/j.chembiol.2014.07.003 Copyright © 2014 Elsevier Ltd Terms and Conditions

Figure 1 Differential Effects of BET Inhibitors on Oligodendrocyte Differentiation (A) Human BET family proteins. The evolutionarily conserved regions, including bromodomain I (BD1), bromodomain II (BD2), extraterminal domain (ET), C-terminal motif (CTM), N-terminal cluster of CK2 phosphorylation sites (NPS), and basic residues-enriched interaction domain (BID) are schematized with conserved N140 and N433 as well as diverged D144 and H437 residues between BD1 and BD2 also indicated. The full-length long (L) and two short (S) forms (a and b) of human BRD4 with common amino acids 1–719 but different 3′ regions generated by alternative splicing are also shown. (B) Chemical inhibitors targeting BD1 and/or BD2 of BET proteins. BrD1i and BrD2i are respective BD1-specific and BD2-specific inhibitors, whereas BETi represents broad inhibitors binding to both BD1 and BD2. Acetylated (Ac) histones and transcription factors (TF) binding to BD1 and/or BD2 are indicated on the bottom. (C) BrD1i promotes, but BETi inhibits, oligodendrocyte differentiation. Representative genes expressed in oligodendrocyte progenitor cells and myelin-producing cells are indicated in respective cells in parentheses. Chemistry & Biology 2014 21, 804-806DOI: (10.1016/j.chembiol.2014.07.003) Copyright © 2014 Elsevier Ltd Terms and Conditions