药物与DNA-RNA杂交结构的结合。
Drug binding to DNA x RNA hybrid structures.
作者信息
Wheelhouse Richard T, Chaires Jonathan B
机构信息
School of Pharmacy, University of Bradford, Bradford, West Yorkshire, UK.
出版信息
Methods Mol Biol. 2010;613:55-70. doi: 10.1007/978-1-60327-418-0_4.
Abstract
The DNA x RNA hybrid duplexes are functionally important structures in gene expression that are underutilized as potential drug targets. Several tools are described here for the discovery and characterization of small molecules capable of the selective recognition of DNA x RNA hybrid structures. Competition dialysis and thermal denaturation of mixtures of polynucleotide structures can be used to identify small molecules that bind selectively to DNA x RNA hybrids. An assay that measures small molecule inhibition of RNase H can be used to measure a functional response to these ligands.
摘要
DNA与RNA杂交双链体是基因表达中功能重要的结构，但作为潜在药物靶点却未得到充分利用。本文介绍了几种用于发现和表征能够选择性识别DNA与RNA杂交结构的小分子的工具。多核苷酸结构混合物的竞争透析和热变性可用于鉴定选择性结合DNA与RNA杂交体的小分子。一种测量小分子对核糖核酸酶H抑制作用的测定法可用于测量对这些配体的功能反应。
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