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US 2022/0175736 A1Published application
Small molecule inhibitors of bacterial efflux pumps and methods of using same
AssigneeThe Regents of the University of Colorado
InventorsAbigail L. Reens, Amy L. Crooks, Corrella S. Detweiler
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Abstract
An empirical Screen for Anti-infectives using Fluorescence microscopy of IntracellulaR Enterobacteriaceae (SAFIRE) was developed. Using this methodology, a library of small molecules and identified antimicrobials that are cell permeable and non-host-toxic were screened. Inhibitors of bacterial efflux pumps were identified as being implicated in antibiotic resistance and are attractive therapeutic targets for antimicrobials.
Claims11
A method of identifying an anti-infective compound with activity against intracellular pathogens, the method comprising:
- (a) providing a first subset of cells and a second subset of cells;
- (b) infecting the first subset of cells and the second subset of cells with a marker-producing bacteria;
- (c) staining the first subset of cells with a vitality marker;
- (d) obtaining a first value of cellular infectivity;
- (e) contacting the second subset of cells with an anti-infective compound;
- (f) staining the second subset of cells with a vitality marker;
- (g) obtaining a second value of cellular infectivity;
- and
- (h) comparing the first value of cellular infectivity to the second value of cellular infectivity;
- and
- (i) identifying an anti-infective compound, wherein the anti-infective compound is identified when the second value of cellular infectivity is decreased compared to the first value of cellular infectivity.
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Dependencies are inferred from the claim text.