Thienopyrimidinone Derivatives That Inhibit Bacterial tRNA (Guanine37-N1)-Methyltransferase (TrmD) by Restructuring the Active Site with a Tyrosine-Flipping Mechanism
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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
Targeting the Bacterial Epitranscriptome for Antibiotic Development: Discovery of Novel tRNA-(N1G37) Methyltransferase (TrmD) Inhibitors.
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DOI: 10.1021/acsinfecdis.8b00275
Abstract: Bacterial tRNA modification synthesis pathways are critical to cell survival under stress and thus represent ideal mechanism-based targets for antibiotic development. One such target is the tRNA-(N1G37) methyltransferase (TrmD), which is conserved and essential in… read more here.
Keywords: trmd; n1g37 methyltransferase; trna n1g37; antibiotic development ... See more keywords
Crystal structure and catalytic mechanism of the essential m1G37 tRNA methyltransferase TrmD from Pseudomonas aeruginosa.
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DOI: 10.1261/rna.066746.118
Abstract: The tRNA (m1G37) methyltransferase TrmD catalyzes m1G formation at position 37 in many tRNA isoacceptors and is essential in most bacteria, which positions it as a target for antibiotic development. In spite of its crucial… read more here.
Keywords: m1g37; trmd pseudomonas; methyltransferase trmd; trna ... See more keywords