GSK's topoisomerase in the hole

Fluoroquinolone antibiotics work by blocking bacterial topoisomerase IIA, but bacterial resistance to this class of drugs is rising faster than new treatments can be developed.^1-3 Researchers at GlaxoSmithKline plc now have generated a new class of antibacterial compounds that can block the activity of bacterial topoisomerase IIA via a mechanism that is distinct from that of fluoroquinolones.⁴

Bacterial topoisomerase IIA is needed to carry out DNA replication: it works to unwind DNA, cleave the double strands and ligate the broken strands back together. Mutations in the two types of bacterial topoisomerase IIA-DNA gyrase and topoisomerase IV-can cause resistance to fluoroquinolones...