Mycobacterial dihydrofolate reductase inhibitors identified using chemogenomic methods and in vitro validation.

ABSTRACT: The lack of success in target-based screening approaches to the discovery of antibacterial agents has led to reemergence of phenotypic screening as a successful approach of identifying bioactive, antibacterial compounds. A challenge though with this route is then to identify the molecular target(s) and mechanism of action of the hits. This target identification, or deorphanization step, is often essential in further optimization and validation studies. Direct experimental identification of the molecular target of a screening hit is often complex, precisely because the properties and specificity of the hit are not yet optimized against that target, and so many false positives are often obtained. An alternative is to use computational, predictive, approaches to hypothesize a mechanism of act

SUBMITTER: Mugumbate G 

PROVIDER: S-EPMC4370846 | biostudies-literature | 2015

REPOSITORIES: biostudies-literature