2. Academic Validation
  3. Novel Inhibitors of E. coli RecA ATPase Activity

Novel Inhibitors of E. coli RecA ATPase Activity

  • Curr Chem Genomics. 2010 May 26;4:34-42. doi: 10.2174/1875397301004010034.
Jonathan Z Sexton 1,  Tim J Wigle,  Qingping He,  Mark A Hughes,  Ginger R Smith,  Scott F Singleton,  Alfred L Williams,  Li-An Yeh
Affiliations

Affiliation

  • 1 Biomanufacturing Research Institute and Technology Enterprise, North Carolina Central University, Durham, 27707, USA.
PMID: 20648224 DOI: 10.2174/1875397301004010034
Abstract

The Bacterial RecA protein has been implicated as a Bacterial drug target not as an antimicrobial target, but as an adjuvant target with the potential to suppress the mechanism by which bacteria gain drug resistance. In order to identify small molecules that inhibit RecA/ssDNA nucleoprotein filament formation, we have adapted the phosphomolybdate-blue ATPase assay for high throughput screening to determine RecA ATPase activity against a library of 33,600 compounds, which is a selected representation of diverse structure of 350,000. Four distinct chemotypes were represented among the 40 validated hits. SAR and further chemical synthesis is underway to optimize this set of inhibitors to be used as antimicrobial adjuvant agents.

Keywords

ATPase inhibition; Antibiotic resistance; RecA; SOS response.; high throughput screening; microbial drug resistance.

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