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Discovery of the first small-molecule CsrA-RNA interaction inhibitors using biophysical screening technologies.
Maurer, Christine K Fruth, Martina Empting, Martin Avrutina, Olga Hoßmann, Jörn Nadmid, Suvd Gorges, Jan Herrmann, Jennifer Kazmaier, Uli
Maurer, Christine K
Fruth, Martina
Empting, Martin
Avrutina, Olga
Hoßmann, Jörn
Nadmid, Suvd
Gorges, Jan
Herrmann, Jennifer
Kazmaier, Uli
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2016-06
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Abstract
CsrA is a global post-transcriptional regulator protein affecting mRNA translation and/or stability. Widespread among bacteria, it is essential for their full virulence and thus represents a promising anti-infective drug target. Therefore, we aimed at the discovery of CsrA-RNA interaction inhibitors. Results & methodology: We followed two strategies: a screening of small molecules (A) and an RNA ligand-based approach (B). Using surface plasmon resonance-based binding and fluorescence polarization-based competition assays, (A) yielded seven small-molecule inhibitors, among them MM14 (IC50 of 4 µM). (B) resulted in RNA-based inhibitor GGARNA (IC50 of 113 µM).
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Discovery of the first small-molecule CsrA-RNA interaction inhibitors using biophysical screening technologies. 2016, 8 (9):931-47 Future Med Chem
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en
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1756-8927