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. Author manuscript; available in PMC: 2020 Jun 25.
Published in final edited form as: Chem Biol. 2010 May 28;17(5):421–433. doi: 10.1016/j.chembiol.2010.04.012

Figure 6. Inhibitors of Type IIA Topoisomerases.

Figure 6.

(A) Inhibitors of eukaryotic Top2 enzymes. All drugs except ICRF-187 trap Top2 cleavage complexes and generate DNA breaks (see Figures 1F–1H). ICRF-187 is a catalytic inhibitor.

(B) Gyrase and Topo IV inhibitors from the quinolone family. All drugs trap cleavage complexes. Note that the quinolone CP-115,953 traps both eukaryotic and prokaryotic enzymes, which is not the case in the other quinolones shown in this panel. Also note that TAS-103 is a dual inhibitor of Top1 and Top2 (Wilson Byl et al., 1999).

(C) Gyrase catalytic inhibitors.