Catalytic metallodrugs targeting HCV IRES RNA

被引:38
作者
Bradford, Seth [1 ]
Cowan, J. A. [1 ,2 ]
机构
[1] Ohio State Univ, Dept Chem, Columbus, OH 43210 USA
[2] MetalloPharm LLC, Delaware, OH 43015 USA
基金
美国国家卫生研究院;
关键词
COPPER(II) TRANSPORT SITE; RESPONSE ELEMENT RNA; ATCUN MOTIF; COMPLEX; ALBUMIN; INACTIVATION; DERMORPHIN; INFECTION; RESIDUES; CLEAVAGE;
D O I
10.1039/c2cc17377h
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A catalytic metallodrug that targets stem-loop IIb of the internal ribosomal entry site (IRES) RNA of hepatitis C virus (HCV) demonstrates enzyme-like turnover with K-M of 0.85 mu M, k(cat) of 0.53 min(-1), and a turnover number of 31.9 for Cu center dot GGHYrFK-amide (1-Cu), and yielded an antiviral activity (IC50) of 0.58 mu M in an HCV cellular replicon assay.
引用
收藏
页码:3118 / 3120
页数:3
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