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. Author manuscript; available in PMC: 2023 Apr 11.
Published in final edited form as: J Med Chem. 2021 May 19;64(11):7617–7629. doi: 10.1021/acs.jmedchem.1c00318

Figure 3.

Figure 3.

(A) Induction of TOP1–DNA covalent cleavage complexes by in vivo complex of enzyme assay in MCF-7 cells. Lane 1, untreated control; lanes 2 and 3, cells treated with TPT at 25 and 50 μM, respectively; lanes 4–6, cells treated with C12 at 25, 50, and 100 μM, respectively. (B) Hypothetical binding mode of C12 in the ternary TOP1–DNA–drug cleavage complex (PDB: 1K4T). (C) Induction of TDP1-DNA covalent complex by ICE assay in MCF-7 and MCF-7/TDP1 cells. Lane 1, untreated control; lanes 2–4, cells treated with TPT (10 μM) and C12 at 10 and 100 μM, respectively; lanes 5 and 6, cells cotreated with TPT (10 μM) and C12 (10 and 100 μM).