HTS model for Poly(ADP-ribose) polymerase-1 inhibitors
- VernacularTitle:聚腺苷二磷酸核糖聚合酶-1抑制剂高通量筛选模型
- Author:
Jun LIU
;
Luyong ZHANG
- Publication Type:Journal Article
- Keywords:
PARP-1;
inhibitor;
high throughput screening(HTS)
- From:
Chinese Pharmacological Bulletin
1987;0(01):-
- CountryChina
- Language:Chinese
-
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.
