Identification and mechanism of action analysis of the new PARP-1 inhibitor 2″-hydroxygenkwanol A.

Fabrizio Dal Piaz,Piera Ferro,Antonio Vassallo,Michele Vasaturo,Giovanni Forte,Maria Giovanna Chini,Giuseppe Bifulco,Alessandra Tosco,Nunziatina De Tommasi

Biochimica et Biophysica Acta (BBA) - General Subjects（2015）

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摘要

•We demonstrated that dimeric spiro-flavonoids bind PARP-1.•2″-hydroxygenkwanol A efficiently modulates PARP-1 both in vitro and in cell.•This molecule binds the nicotine binding pocket of the protein.•It represents a promising lead for the design of a new class of PARP-1 inhibitors.

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PARP-1,NAD+,SPR,MS

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