A Fragment-Based Approach to Identifying Ligands for Riboswitches

被引：41

作者：

Chen, Liuhong ^{[1
]}

Cressina, Elena ^{[2
]}

Leeper, Finian J. ^{[1
]}

Smith, Alison G. ^{[2
]}

Abell, Chris ^{[1
]}

机构：

[1] Univ Cambridge, Dept Chem, Cambridge CB2 1EW, England

[2] Univ Cambridge, Dept Plant Sci, Cambridge CB2 3EA, England

来源：

ACS CHEMICAL BIOLOGY | 2010年 / 5卷 / 04期

基金：

英国生物技术与生命科学研究理事会;

关键词：

BACTERIAL GENE-EXPRESSION; DRUG DISCOVERY; RNA; BIOSYNTHESIS; DESIGN;

D O I：

10.1021/cb9003139

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：

Riboswitches are regions of mRNA that directly bind metabolites, leading to alteration of gene expression. We have developed fragment-based methods to screen for compounds that bind the Escherichia coli thiM riboswitch. Using complementary biophysical techniques we have identified several ligands with K-D <100 mu M. From these there is the potential to develop potent and selective modulators of riboswitch function.

引用

页码：355 / 358

页数：4

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