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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...
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. |
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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 |
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