Abstract

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Liuhong Chen, Elena Cressina, Finian J. Leeper, Alison G. Smith and Chris Abell, “A Fragment-Based Approach to Identifying Ligands for Riboswitches” ACS Chem. Biol., 2010, 5 (4), 355-358. Full Text.

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 coil thiM riboswitch. Using complementary biophysical techniques we have identified several ligands with K_D <100 mM. From these there is the potential to develop potent and selective modulators of riboswitch function.

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