Structure–activity relationship studies of c-di-AMP synthase inhibitor, bromophenol-thiohydantoin

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

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-...

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Cyclic di-adenosine monophosphate (c-di-AMP) is a recently discovered bacterial second messenger implicated in the control of cell wall metabolism, osmotic stress responses and sporulation. However, the mechanisms by which c-di-AMP triggers these physiological responses have remained largely unknown. Notably, a candidate riboswitch class called ydaO associates with numerous genes involved in th...

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Crystal structure of the c-di-AMP riboswitch reveals an internally pseudo-dimeric RNA

In addition, while we realize that going much further into the functional validation of c-di-AMP binding in vivo as requested by ref #1 (point 1) may be outside the scope of the current study, we would encourage you to include any data that you may have to address that point. However, while such additional insight would certainly strengthen the current manuscript, it is not an absolute requirem...

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ژورنال

عنوان ژورنال: Tetrahedron

سال: 2016

ISSN: 0040-4020

DOI: 10.1016/j.tet.2015.10.073