Ontology highlight
ABSTRACT:
SUBMITTER: Krajnc A
PROVIDER: S-EPMC6767355 | biostudies-literature | 2019 Sep
REPOSITORIES: biostudies-literature
Krajnc Alen A Brem Jürgen J Hinchliffe Philip P Calvopiña Karina K Panduwawala Tharindi D TD Lang Pauline A PA Kamps Jos J A G JJAG Tyrrell Jonathan M JM Widlake Emma E Saward Benjamin G BG Walsh Timothy R TR Spencer James J Schofield Christopher J CJ
Journal of medicinal chemistry 20190916 18
The bicyclic boronate VNRX-5133 (taniborbactam) is a new type of β-lactamase inhibitor in clinical development. We report that VNRX-5133 inhibits serine-β-lactamases (SBLs) and some clinically important metallo-β-lactamases (MBLs), including NDM-1 and VIM-1/2. VNRX-5133 activity against IMP-1 and tested B2/B3 MBLs was lower/not observed. Crystallography reveals how VNRX-5133 binds to the class D SBL OXA-10 and MBL NDM-1. The crystallographic results highlight the ability of bicyclic boronates to ...[more]