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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
来源:
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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