A Fragment-Based Approach to Identifying Ligands for Riboswitches

作者:Chen Liuhong; Cressina Elena; Leeper Finian J; Smith Alison G; Abell Chris*
来源:ACS Chemical Biology, 2010, 5(4): 355-358.
DOI:10.1021/cb9003139

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.

  • 出版日期2010-4