Bioluminescent Reporters for Rapid Mechanism of Action Assessment in Tuberculosis Drug Discovery.

ABSTRACT: The tuberculosis (TB) drug discovery pipeline is fueled by compounds identified in whole-cell screens against the causative agent, Mycobacterium tuberculosis Phenotypic screening enables the selection of molecules that inhibit essential cellular functions in live, intact bacilli grown under a chosen in vitro condition. However, deducing the mechanism of action (MOA), which is important to avoid promiscuous targets, often requires significant biological resources in a lengthy process that risks decoupling medicinal chemistry and biology efforts. Therefore, there is a need to develop methods enabling rapid MOA assessment of putative "actives" for triage decisions. Here, we describe a modified version of a bioluminescence reporter assay that allows nondestructive detection of compounds target

SUBMITTER: Naran K 

PROVIDER: S-EPMC5075082 | biostudies-literature | 2016 Nov

REPOSITORIES: biostudies-literature