HTS model for Poly(ADP-ribose) polymerase-1 inhibitors / 中国药理学通报

ABSTRACT

Aim To introduce a high throughput screen model for PARP-1 inhibitors. Methods Setting up an assay for PARP-1 activity relies on the conversion of NAD~+into a highly fluorescent compound. The inhibitory effects of 9 280 samples(including pure organic compounds, extracts from plants and extracts from microorganism)were screened by the high throughout assay. Results 148 compounds had inhibitory effects over 70%. Ultimately, three inhibitors were identified as PARP-1 inhibitor with high activity.Conclusion The high throughput screening was a highly sensitive, inexpensive, and operationally simple assay method in identifying PARP-1 inhibitors.