| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10591942 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
Poly(ADP-ribose)polymerase-1 (PARP-1) enzyme is involved in the repair of DNA damages made by certain anticancer agents. It is suggested that PARP-1 inhibitors potentiate the cytotoxic effects and circumvent the resistance of DNA-modifying anticancer agents such as cisplatin. In this study, we conducted virtual screening of Korea Chemical Bank database targeting PARP-1 and identified several potent PARP-1 inhibitors with submicromolar IC50 values (77-79Â nM). We then examined the chemosensitization of cisplatin by pre-treatment of PARP-1 inhibitors in cisplatin-resistant human gastric cancer cells. Our results show that PARP-1 inhibitors suppress the formation of poly(ADP-ribose) and enhance the cytotoxicity of cisplatin.
Related Topics
Physical Sciences and Engineering
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Authors
Tuong Vy Thi Le, Jee Hee Suh, Nakjeong Kim, Hyun-Ju Park,