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Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction

[Image: see text] A novel series of histone deacetylase (HDAC) inhibitors lacking a zinc-binding moiety has been developed and described herein. HDAC isozyme profiling and kinetic studies indicate that these inhibitors display a selectivity preference for HDACs 1, 2, 3, 10, and 11 via a rapid equili...

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Detalles Bibliográficos
Autores principales: Beshore, Douglas C., Adam, Gregory C., Barnard, Richard J. O., Burlein, Christine, Gallicchio, Steven N., Holloway, M. Katharine, Krosky, Daniel, Lemaire, Wei, Myers, Robert W., Patel, Sangita, Plotkin, Michael A., Powell, David A., Rada, Vanessa, Cox, Christopher D., Coleman, Paul J., Klein, Daniel J., Wolkenberg, Scott E.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2021
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8040053/
https://www.ncbi.nlm.nih.gov/pubmed/33854701
http://dx.doi.org/10.1021/acsmedchemlett.1c00074