Journal
DYES AND PIGMENTS
Volume 169, Issue -, Pages 45-50Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.dyepig.2019.05.010
Keywords
Tyrosyl-DNA phosphodiesterase; Fluorescent probe; DNA repair; Inhibitor
Funding
- National Natural Science Foundation of China [81373257]
- Guangdong Provincial Key Laboratory of Construction Foundation [2017B030314030]
- Medical Scientific Research Foundation of Guangdong Province [A2017051]
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Tyrosyl-DNA phosphodiesterase 1 (TDP1) is a recently discovered enzyme specifically repairing DNA topoisomerase IB-mediated DNA damage, and is a rational anticancer target. Herein, we report the design and synthesis of the first small fluorescent probe 1 as TDP1 substrate. Probe 1 is a specific substrate of TDP1 and shows good spectroscopic properties with more than 140-fold fluorescence enhancement. A novel TDP1 inhibition assay was established using 1 as substrate. The possible cleavage pathway of 1 by TDP1 was also studied.
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