期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 9, 页码 2642-2646出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.02.094
关键词
Cisplatin-resistance; PARP-1 inhibitor; Chemosensitization
资金
- Basic Science Research Program through the National Research Foundation of Korea(NRF)
- Ministry of Education, Science and Technology [2010-0029358]
- Korea Healthcare technology R&D Project, Ministry for Health & Welfare, Republic of Korea [A092006]
- National Research Foundation of Korea [2012R1A5A2A28671860, 2010-0029358] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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 (77-79 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. (C) 2013 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据