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1. Identification of bromophenol thiohydantoin as an inhibitor of DisA, a c-di-AMP synthase, from a 1000 compound library, using the coralyne assay.

Author

Zheng Y, Zhou J, Sayre DA, and Sintim HO

Subjects
Berberine Alkaloids analysis, Dose-Response Relationship, Drug, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors chemistry, Enzyme Inhibitors isolation & purification, Molecular Structure, Nucleotidyltransferases metabolism, Phenols chemical synthesis, Phenols chemistry, Small Molecule Libraries chemical synthesis, Small Molecule Libraries chemistry, Structure-Activity Relationship, Berberine Alkaloids chemistry, Dinucleoside Phosphates biosynthesis, Enzyme Assays, Enzyme Inhibitors pharmacology, Nucleotidyltransferases antagonists & inhibitors, Phenols pharmacology, Small Molecule Libraries pharmacology
Abstract

c-di-AMP is an important bacterial second messenger found in Gram-positive and mycobacteria. c-di-AMP regulates myriads of processes in bacteria as well as immune response in higher organisms so interest in small molecules that would attenuate the activity of c-di-AMP metabolism enzymes is high. Herein, we report the first small molecule inhibitor of a c-di-AMP synthase, DisA, using a coralyne-based assay.

Published
2014
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