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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Main Authors:	Jasmine M. Cross, Tim R. Blower, Alexander D. H. Kingdon, Robert Pal, David M. Picton, James W. Walton
Format:	Article
Language:	English
Published:	MDPI AG 2020-05-01
Series:	Molecules
Subjects:	histone deacetylase inhibitors ruthenium in medicine selective enzyme inhibition
Online Access:	https://www.mdpi.com/1420-3049/25/10/2383

id	doaj-6ca263e9df1147debc04b2066e7b6e4a
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spelling	doaj-6ca263e9df1147debc04b2066e7b6e4a2020-11-25T03:26:34ZengMDPI AGMolecules1420-30492020-05-01252383238310.3390/molecules25102383Anticancer Ruthenium Complexes with HDAC Isoform SelectivityJasmine M. Cross0Tim R. Blower1Alexander D. H. Kingdon2Robert Pal3David M. Picton4James W. Walton5Department of Chemistry, Durham University, Lower Mountjoy, South Road, Durham DH1 3LE, UKDepartment of Biosciences, Durham University, Stockton Road, Durham DH1 3LE, UKDepartment of Chemistry, Durham University, Lower Mountjoy, South Road, Durham DH1 3LE, UKDepartment of Chemistry, Durham University, Lower Mountjoy, South Road, Durham DH1 3LE, UKDepartment of Biosciences, Durham University, Stockton Road, Durham DH1 3LE, UKDepartment of Chemistry, Durham University, Lower Mountjoy, South Road, Durham DH1 3LE, UKThe 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.https://www.mdpi.com/1420-3049/25/10/2383histone deacetylase inhibitorsruthenium in medicineselective enzyme inhibition
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Jasmine M. Cross Tim R. Blower Alexander D. H. Kingdon Robert Pal David M. Picton James W. Walton
spellingShingle	Jasmine M. Cross Tim R. Blower Alexander D. H. Kingdon Robert Pal David M. Picton James W. Walton Anticancer Ruthenium Complexes with HDAC Isoform Selectivity Molecules histone deacetylase inhibitors ruthenium in medicine selective enzyme inhibition
author_facet	Jasmine M. Cross Tim R. Blower Alexander D. H. Kingdon Robert Pal David M. Picton James W. Walton
author_sort	Jasmine M. Cross
title	Anticancer Ruthenium Complexes with HDAC Isoform Selectivity
title_short	Anticancer Ruthenium Complexes with HDAC Isoform Selectivity
title_full	Anticancer Ruthenium Complexes with HDAC Isoform Selectivity
title_fullStr	Anticancer Ruthenium Complexes with HDAC Isoform Selectivity
title_full_unstemmed	Anticancer Ruthenium Complexes with HDAC Isoform Selectivity
title_sort	anticancer ruthenium complexes with hdac isoform selectivity
publisher	MDPI AG
series	Molecules
issn	1420-3049
publishDate	2020-05-01
description	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.
topic	histone deacetylase inhibitors ruthenium in medicine selective enzyme inhibition
url	https://www.mdpi.com/1420-3049/25/10/2383
work_keys_str_mv	AT jasminemcross anticancerrutheniumcomplexeswithhdacisoformselectivity AT timrblower anticancerrutheniumcomplexeswithhdacisoformselectivity AT alexanderdhkingdon anticancerrutheniumcomplexeswithhdacisoformselectivity AT robertpal anticancerrutheniumcomplexeswithhdacisoformselectivity AT davidmpicton anticancerrutheniumcomplexeswithhdacisoformselectivity AT jameswwalton anticancerrutheniumcomplexeswithhdacisoformselectivity
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Anticancer Ruthenium Complexes with HDAC Isoform Selectivity

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