Ontology highlight
ABSTRACT:
SUBMITTER: Tyler DS
PROVIDER: S-EPMC5865750 | biostudies-literature | 2017 Jun
REPOSITORIES: biostudies-literature
Tyler Dean S DS Vappiani Johanna J Cañeque Tatiana T Lam Enid Y N EYN Ward Aoife A Gilan Omer O Chan Yih-Chih YC Hienzsch Antje A Rutkowska Anna A Werner Thilo T Wagner Anne J AJ Lugo Dave D Gregory Richard R Ramirez Molina Cesar C Garton Neil N Wellaway Christopher R CR Jackson Susan S MacPherson Laura L Figueiredo Margarida M Stolzenburg Sabine S Bell Charles C CC House Colin C Dawson Sarah-Jane SJ Hawkins Edwin D ED Drewes Gerard G Prinjha Rab K RK Rodriguez Raphaël R Grandi Paola P Dawson Mark A MA
Science (New York, N.Y.) 20170615 6345
The success of new therapies hinges on our ability to understand their molecular and cellular mechanisms of action. We modified BET bromodomain inhibitors, an epigenetic-based therapy, to create functionally conserved compounds that are amenable to click chemistry and can be used as molecular probes in vitro and in vivo. We used click proteomics and click sequencing to explore the gene regulatory function of BRD4 (bromodomain containing protein 4) and the transcriptional changes induced by BET i ...[more]