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Thienopyrimidinone Derivatives That Inhibit Bacterial tRNA (Guanine37-N1)-Methyltransferase (TrmD) by Restructuring the Active Site with a Tyrosine-Flipping Mechanism

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0 Published in 2019 at "Journal of Medicinal Chemistry"

DOI: 10.1021/acs.jmedchem.9b00582

Abstract: Among the >120 modified ribonucleosides in the prokaryotic epitranscriptome, many tRNA modifications are critical to bacterial survival, which makes their synthetic enzymes ideal targets for antibiotic development. Here we performed a structure-based design of inhibitors… read more here.

Keywords: trmd; thienopyrimidinone derivatives; tyrosine flipping; active site ... See more keywords