A Series of Potent CREBBP Bromodomain Ligands Reveals an Induced-Fit Pocket Stabilized by a Cation–π Interaction**

The benzoxazinone and dihydroquinoxalinone fragments were employed as novel acetyl lysine mimics in the development of CREBBP bromodomain ligands. While the benzoxazinone series showed low affinity for the CREBBP bromodomain, expansion of the dihydroquinoxalinone series resulted in the first potent...

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Detalles Bibliográficos
Autores principales: Rooney, Timothy P C, Filippakopoulos, Panagis, Fedorov, Oleg, Picaud, Sarah, Cortopassi, Wilian A, Hay, Duncan A, Martin, Sarah, Tumber, Anthony, Rogers, Catherine M, Philpott, Martin, Wang, Minghua, Thompson, Amber L, Heightman, Tom D, Pryde, David C, Cook, Andrew, Paton, Robert S, Müller, Susanne, Knapp, Stefan, Brennan, Paul E, Conway, Stuart J
Formato: Online Artículo Texto
Lenguaje:English
Publicado: WILEY-VCH Verlag 2014
Materias:
Communications
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4298791/
https://www.ncbi.nlm.nih.gov/pubmed/24821300
http://dx.doi.org/10.1002/anie.201402750

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