Anticancer Ruthenium Complexes with HDAC Isoform Selectivity

被引:10
作者
Cross, Jasmine M. [1 ]
Blower, Tim R. [2 ]
Kingdon, Alexander D. H. [1 ]
Pal, Robert [1 ]
Picton, David M. [2 ]
Walton, James W. [1 ]
机构
[1] Univ Durham, Dept Chem, South Rd, Durham DH1 3LE, England
[2] Univ Durham, Dept Biosci, Stockton Rd, Durham DH1 3LE, England
关键词
histone deacetylase inhibitors; ruthenium in medicine; selective enzyme inhibition; HISTONE DEACETYLASE INHIBITOR; METAL-COMPLEXES; RATIONAL DESIGN; MOLECULAR-BASIS; CELL-GROWTH; MECHANISM;
D O I
10.3390/molecules25102383
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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.
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页数:8
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