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| BTH-8, a novel poly (ADP-ribose) polymerase-1 (PARP-1) inhibitor, causes DNA double-strand breaks and exhibits anticancer activities in vitro and in vivo | |
| Guo, Chuanlong1,2; Zhang, Fan1,2; Wu, Xiaochen1,2; Yu, Xuemin3,4; Wu, Xianggen1,2; Shi, Dayong6; Wang, Lijun5,7 | |
| 2020-05-01 | |
| 发表期刊 | INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
 |
| ISSN | 0141-8130 |
| 卷号 | 150页码:238-245 |
| 通讯作者 | Guo, Chuanlong(guochuanlong@qust.edu.cn) ; Shi, Dayong(shidayong@sdu.edu.cn) ; Wang, Lijun(wanglijun@qdio.ac.cn) |
| 摘要 | Poly (ADP-ribose) polymerase (PARP) is a family of enzymes that play an important role in DNA repair. We designed 2-(2,3,6-tribromo-4,5-dimethoxybenzylidene) hydrazinecarbothioamide (BTH-8) as a novel human PARP (PARP-1) inhibitor with anticancer activities in vitro and in vivo. With an IC50 value of 79.79 +/- 2.16 nM, BTH-8 caused DNA double-strand breaks, increased the foci quantitation of gamma-H2AX and inhibited poly(ADP-ribose) (PAR) formation. BTH-8 could bind to PARP-1 with the target affinity [KD (equilibrium dissociation constant) value] of 1.372 mu M. BTH-8 can inhibit the proliferation of a variety of tumor cells, especially BRCA-deficient cells (HCC-1937 and Capan-1). Further investigation showed that BTH-8 effectively induced a significant amount of G2/Mcell cycle arrest and cell apoptosis in HCC-1937 cells. BTH-8 also exhibited antitumor activity in vivo, which was achieved by the inhibition of PARP-1. In sum, our study indicates that BTH-8 might be a novel suitable PARP-1 inhibitor to treat human breast cancer. (C) 2020 Elsevier B.V. All rights reserved. |
| 关键词 | PARP-1 inhibitor DNA double-strand breaks HCC-1937 In vivo Apoptosis |
| DOI | 10.1016/j.ijbiomac.2020.02.069 |
| 收录类别 | SCI |
| 语种 | 英语 |
| 资助项目 | National Natural Science Foundation of China[81773586] ; Talent Fund of Shandong Collaborative Innovation Center of Eco-Chemical Engineering[XTCXQN19] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry ; Polymer Science |
| WOS类目 | Biochemistry & Molecular Biology ; Chemistry, Applied ; Polymer Science |
| WOS记录号 | WOS:000525869500025 |
| 出版者 | ELSEVIER |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.qdio.ac.cn/handle/337002/167176 |
| 专题 | 实验海洋生物学重点实验室 |
| 通讯作者 | Guo, Chuanlong; Shi, Dayong; Wang, Lijun |
| 作者单位 | 1.Qingdao Univ Sci & Technol, Dept Pharm, Coll Chem Engn, Qingdao 266042, Peoples R China 2.Qingdao Univ Sci & Technol, Key Lab Pharmaceut Res Metab Dis, Qingdao 266042, Peoples R China 3.Shandong Univ, Dept Otorhinolaryngol, Qilu Hosp, Qingdao 266035, Shandong, Peoples R China 4.NHC Key Lab Otorhinolaryngol, Qingdao 266035, Shandong, Peoples R China 5.Chinese Acad Sci, Inst Oceanol, CAS Key Lab Expt Marine Biol, Qingdao 266071, Peoples R China 6.Shandong Univ, State Key Lab Microbial Technol, Qingdao 266273, Shandong, Peoples R China 7.Chinese Acad Sci, Ctr Ocean Mega Sci, 7 Nanhai Rd, Qingdao 266071, Peoples R China |
| 通讯作者单位 | 中国科学院海洋研究所 |
| 推荐引用方式 GB/T 7714 | Guo, Chuanlong,Zhang, Fan,Wu, Xiaochen,et al. BTH-8, a novel poly (ADP-ribose) polymerase-1 (PARP-1) inhibitor, causes DNA double-strand breaks and exhibits anticancer activities in vitro and in vivo[J]. INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,2020,150:238-245. |
| APA | Guo, Chuanlong.,Zhang, Fan.,Wu, Xiaochen.,Yu, Xuemin.,Wu, Xianggen.,...&Wang, Lijun.(2020).BTH-8, a novel poly (ADP-ribose) polymerase-1 (PARP-1) inhibitor, causes DNA double-strand breaks and exhibits anticancer activities in vitro and in vivo.INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,150,238-245. |
| MLA | Guo, Chuanlong,et al."BTH-8, a novel poly (ADP-ribose) polymerase-1 (PARP-1) inhibitor, causes DNA double-strand breaks and exhibits anticancer activities in vitro and in vivo".INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES 150(2020):238-245. |
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