Herein, we report a novel whole-cell screening assay {using|utilizing|making use of|employing|working with|applying} Lactobacillus casei as model microorganism to {identify|determine|recognize} inhibitors of energy-coupling {factor|aspect|element|issue} (ECF) transporters. This promising and underexplored target {may have|might have} {important|essential|crucial|critical|significant|vital} pharmacological {potential|possible|prospective} {through|via|by means of|by way of} modulation of vitamin homeostasis in bacteria and, importantly, {it is|it’s|it really is|it truly is|it can be|it is actually} absent in humans. The assay represents an {alternative|option}, cost-effective and {fast|quick|quickly|rapidly|rapid|speedy} {solution|answer|remedy|resolution|option} to demonstrate the direct involvement {of these|of those} membrane transporters {in a|inside a|within a} native biological {environment|atmosphere} {rather than|instead of|as opposed to|as an alternative to|in lieu of} {using|utilizing|making use of|employing|working with|applying} a low-throughput in vitro assay employing reconstituted proteins {in a|inside a|within a} membrane bilayer {system|method|program|technique}. {Based|Primarily based} on this new whole-cell screening {approach|method|strategy}, we demonstrated the optimization of a weak hit compound ({2|two}) into a {small|little|tiny|modest|smaller|compact} molecule ({3|three}) with {improved|enhanced} in vitro and whole-cell activities. This study opens the possibility to {quickly|rapidly|swiftly|speedily|promptly|immediately} {identify|determine|recognize} novel inhibitors of ECF transporters and optimize them {based|primarily based} on structure–activity relationships. 2377610-54-1 Purity (S)-(-)-tert-Butylsulfinamide Order PMID:23800738
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