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Directed molecular screening for RecA ATPase inhibitors
Tim J Wigle1, Scott F Singleton
1School of Pharmacy, Division of Medicinal Chemistry and Natural Products, The University of North Carolina at Chapel Hill, CB #7360, Chapel Hill, NC 27599-7360, USA.
Bioorganic & Medicinal Chemistry Letters
|May 15, 2007
Summary
Bacterial RecA protein is crucial for antibiotic resistance gene spread. Researchers screened compounds using fluorescence assays, finding three suramin-like agents significantly inhibited RecA
Area of Science:
- Microbiology
- Biochemistry
- Drug Discovery
Background:
- Bacterial RecA protein plays a key role in the evolution and transmission of antibiotic resistance genes.
- Targeting RecA with small molecules presents a promising strategy to combat antibiotic resistance.
Purpose of the Study:
- To screen for small molecule inhibitors of bacterial RecA's ATPase activity.
- To identify novel chemical scaffolds that can inhibit RecA function.
Main Methods:
- Development and utilization of two complementary fluorescence-based ATPase assays for RecA inhibition screening.
- Optimization of an ADP-linked ATPase assay in 96-well microplates with a Z' factor of 0.83.
- Screening of 18 select compounds from five related inhibitor scaffolds against RecA ATPase activity.
Main Results:
- Nucleotide analogs, GHL ATPase inhibitors, and protein kinase inhibitors showed no significant inhibition of RecA ATPase activity.
- Three suramin-like agents demonstrated substantial inhibition of RecA's ATP hydrolysis.
- The ADP-linked ATPase assay proved effective for high-throughput screening of RecA inhibitors.
Conclusions:
- Suramin-like compounds are identified as potent inhibitors of bacterial RecA ATPase activity.
- This study validates fluorescence-based ATPase assays for discovering novel RecA inhibitors.
- Targeting bacterial RecA offers a potential avenue for developing new strategies against antibiotic resistance.
