Fluorescent peptide displacement as a general assay for screening small molecule libraries against RNA

被引：29
|
作者：
Patwardhan, Neeraj N. [1 ]
Cai, Zhengguo [1 ]
Newson, Colby N. [1 ]
Hargrove, Amanda E. [1 ]
机构：
[1] Dept Chem, 124 Sci Dr,Box 90346, Durham, NC 27708 USA
来源：
ORGANIC & BIOMOLECULAR CHEMISTRY | 2019年 / 17卷 / 07期
关键词：
HIV-1 TAR RNA; BINDING SMALL MOLECULES; BIOACTIVE SMALL MOLECULES; SEQUENCE-BASED DESIGN; REV-RRE INTERACTION; AMINOGLYCOSIDE BINDING; DECODING REGION; A-SITE; DISCOVERY; RECOGNITION;
D O I：
10.1039/c8ob02467g
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A prominent hurdle in developing small molecule probes against RNA is the relative scarcity of general screening methods. In this study, we demonstrate the application of a fluorescent peptide displacement assay to screen small molecule probes against four different RNA targets. The designed experimental protocol combined with statistical analysis provides a fast and convenient method to simultaneously evaluate small molecule libraries against different RNA targets and classify them based on affinity and selectivity patterns.
引用
收藏
页码：1778 / 1786
页数：9
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