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A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain

Research into the chemical biology of bromodomains has been driven by the development of acetyl-lysine mimetics. The ligands are typically anchored by binding to a highly conserved asparagine residue. Atypical bromodomains, for which the asparagine is mutated, have thus far proven elusive targets, i...

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Detalles Bibliográficos
Autores principales: Cox, Oakley B., Krojer, Tobias, Collins, Patrick, Monteiro, Octovia, Talon, Romain, Bradley, Anthony, Fedorov, Oleg, Amin, Jahangir, Marsden, Brian D., Spencer, John, von Delft, Frank, Brennan, Paul E.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Royal Society of Chemistry 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5977933/
https://www.ncbi.nlm.nih.gov/pubmed/29910922
http://dx.doi.org/10.1039/c5sc03115j