AI Article Synopsis
- CsrA is an important regulator protein that impacts how bacteria manage their mRNA, playing a key role in their ability to cause infections, making it a target for new drugs.
- The research involved two main methods: screening small molecules, which found seven inhibitors including one with significant potency, and an RNA-based approach that identified an RNA inhibitor with moderate effectiveness.
- The discovery of these small-molecule inhibitors provides a new avenue to explore how inhibiting CsrA-RNA interactions can affect bacterial virulence, paving the way for potential treatments.
Article Abstract
Aim: 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).
Conclusion: The first small-molecule inhibitors of the CsrA-RNA interaction were discovered exhibiting micromolar affinities. These hits represent tools to investigate the effects of CsrA-RNA interaction inhibition on bacterial virulence.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.4155/fmc-2016-0033 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!