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Antibacterial Strategy against H. pylori: Inhibition of the Radical SAM Enzyme MqnE in Menaquinone Biosynthesis.

ABSTRACT: Aminofutalosine synthase (MqnE) catalyzes an important rearrangement reaction in menaquinone biosynthesis by the futalosine pathway. In this Letter, we report the identification of previously unreported inhibitors of MqnE using a mechanism-guided approach. The best inhibitor shows efficient inhibitory activity against H. pylori (IC50 = 1.8 ± 0.4 ?M) and identifies MqnE as a promising target for antibiotic development.

SUBMITTER: Joshi S 

PROVIDER: S-EPMC6421580 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature

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Antibacterial Strategy against <i>H. pylori</i>: Inhibition of the Radical SAM Enzyme MqnE in Menaquinone Biosynthesis.

Joshi Sumedh S   Fedoseyenko Dmytro D   Mahanta Nilkamal N   Ducati Rodrigo G RG   Feng Mu M   Schramm Vern L VL   Begley Tadhg P TP  

ACS medicinal chemistry letters 20190215 3

Aminofutalosine synthase (MqnE) catalyzes an important rearrangement reaction in menaquinone biosynthesis by the futalosine pathway. In this Letter, we report the identification of previously unreported inhibitors of MqnE using a mechanism-guided approach. The best inhibitor shows efficient inhibitory activity against <i>H. pylori</i> (IC<sub>50</sub> = 1.8 ± 0.4 μM) and identifies MqnE as a promising target for antibiotic development. ...[more]

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