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Anticancer Ruthenium Complexes with HDAC Isoform Selectivity.


ABSTRACT: 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.

SUBMITTER: Cross JM 

PROVIDER: S-EPMC7287671 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature

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Anticancer Ruthenium Complexes with HDAC Isoform Selectivity.

Cross Jasmine M JM   Blower Tim R TR   Kingdon Alexander D H ADH   Pal Robert R   Picton David M DM   Walton James W JW  

Molecules (Basel, Switzerland) 20200521 10


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. ...[more]

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