Ontology highlight
ABSTRACT:
SUBMITTER: Kolaric A
PROVIDER: S-EPMC7794245 | biostudies-literature | 2021 Jan
REPOSITORIES: biostudies-literature
Nature communications 20210108 1
Novel bacterial type II topoisomerase inhibitors (NBTIs) stabilize single-strand DNA cleavage breaks by DNA gyrase but their exact mechanism of action has remained hypothetical until now. We have designed a small library of NBTIs with an improved DNA gyrase-binding moiety resulting in low nanomolar inhibition and very potent antibacterial activity. They stabilize single-stranded cleavage complexes and, importantly, we have obtained the crystal structure where an NBTI binds gyrase-DNA in a single ...[more]