Fig. 9: TDP1 catalytic reaction and representative gel images. | Communications Chemistry

Fig. 9: TDP1 catalytic reaction and representative gel images.

From: Targeted sulfur(VI) fluoride exchange-mediated covalent modification of a tyrosine residue in the catalytic pocket of tyrosyl-DNA phosphodiesterase 1

Fig. 9

a Scheme of the TDP1 catalytic reaction applied in the gel assays. Cy5-N14Y and Cy5-N14P are the substrate and product of TDP1, respectively. b Representative gels showing the inhibition of full-length TDP1-catalyzed hydrolysis by quinolines 2a, 2e, 2f and 3a, 3c – g. In each gel: lane 1, DNA (Cy5-N14Y) alone; lane 2, DNA and recombinant TDP1; lanes 3–10, DNA, recombinant TDP1 and the active compounds at 3-fold serial dilution of tested drugs; for 2a and 3a: 3-fold serial dilution of drugs from 12 μM to 27 mM; for 2e, 2f, 3c – g: 3-fold serial dilution of drugs from 4 μM to 9 mM.

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