Click chemistry enables preclinical evaluation of targeted epigenetic therapies

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...

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Published in:Science
Main Authors: Tyler, Dean S., Vappiani, Johanna, Cañeque, Tatiana, Lam, Enid Y. N., Ward, Aoife, Gilan, Omer, Chan, Yih-Chih, Hienzsch, Antje, Rutkowska, Anna, Werner, Thilo, Wagner, Anne J., Lugo, Dave, Gregory, Richard, Molina, Cesar Ramirez, Garton, Neil, Wellaway, Christopher R., Jackson, Susan, MacPherson, Laura, Figueiredo, Margarida, Stolzenburg, Sabine, Bell, Charles C., House, Colin, Dawson, Sarah-Jane, Hawkins, Edwin D., Drewes, Gerard, Prinjha, Rab K., Rodriguez, Raphaël, Grandi, Paola, Dawson, Mark A.
Format: Artigo
Language:Inglês
Published: 2017
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Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC5865750/
https://ncbi.nlm.nih.gov/pubmed/28619718
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1126/science.aal2066
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