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Anticancer Ruthenium Complexes with HDAC Isoform Selectivity

The histone deacetylase (HDAC) enzymes have emerged as an important class of molecular targets in cancer therapy, with five inhibitors in clinical use. Recently, it has been shown that a lack of selectivity between the 11 Zn-dependent HDAC isoforms may lead to unwanted side-effects. In this paper, w...

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Detalles Bibliográficos
Autores principales: Cross, Jasmine M., Blower, Tim R., Kingdon, Alexander D. H., Pal, Robert, Picton, David M., Walton, James W.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7287671/
https://www.ncbi.nlm.nih.gov/pubmed/32455529
http://dx.doi.org/10.3390/molecules25102383
Descripción
Sumario:The histone deacetylase (HDAC) enzymes have emerged as an important class of molecular targets in cancer therapy, with five inhibitors in clinical use. Recently, it has been shown that a lack of selectivity between the 11 Zn-dependent HDAC isoforms may lead to unwanted side-effects. In this paper, we show that piano stool Ru complexes can act as HDAC inhibitors, and variation in the capping arene leads to differences in HDAC isoform selectivity.