Molecular Tweezers Inhibit PARP‐1 by a New Mechanism

2017 
Inhibition of the key enzyme for DNA quality control, i.e. PARP-1, by synthetic molecular tweezers is demonstrated via a non-competitive mechanism with an IC50 value of 3 µM. Electrophoretic mobility shift assays and molecular docking experiments point to a simultaneous inclusion of lysine side chains in the tweezers cavity and one phosphate arm to the central Zn2+ ion of the zinc finger thereby displacing DNA.Abstract Text, 800-1000 characters.
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