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：

MOLECULES | 2020年 / 25卷 / 10期

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.

引用

页数：8

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