YHHU0895, a novel synthetic small-molecule microtubule-destabilizing agent, effectively overcomes P-glycoprotein-mediated tumor multidrug resistance
文献类型：期刊论文
| 作者 | Zhao, Hongbing; Quan, Haitian ; Xie, Chengying; Xu, Yongping; Xie, Fuchun; Hu, Youhong; Lou, Liguang
|
| 刊名 | CANCER LETTERS
 |
| 出版日期 | 2012 |
| 卷号 | 314期号:1页码:54-62 |
| 关键词 | YHHU0895 Microtubule P-glycoprotein Multidrug resistance Microtubule-destabilizing agent |
| ISSN号 | 0304-3835 |
| DOI | 10.1016/j.canlet.2011.09.013 |
| 文献子类 | Article |
| 英文摘要 | P-glycoprotein-mediated multidrug resistance (MDR) is a major limiting factor in the efficacy of most microtubule-targeting agents. Here, we investigated the novel, synthetic, and small-molecule microtubule-destabilizing agent, 2-(2-amino-5-(1-ethyl-1H-indol-5-yl) pyrimidin-4-yl) phenol (YHHU0895), for its anti-tumor activity and potential for overcoming P-glycoprotein-mediated MDR. YHHU0895 inhibited purified tubulin polymerization through binding to tubulin at the colchicine-binding site and significantly inhibited human tumor cell proliferation. Notably, P-glycoprotein-overexpressing KBV200 and K562/ADR cells, which are strongly resistant to colchicine, vinorelbine and paclitaxel, were sensitive to YHHU0895 both in vitro and in vivo. These findings indicate that YHHU0895 is a novel type of microtubule-destabilizing agent that has the potential for the treatment of patients with drug resistance mediated by P-glycoprotein. (C) 2011 Elsevier Ireland Ltd. All rights reserved. |
| WOS关键词 | DRUG-RESISTANCE ; TUBULIN POLYMERIZATION ; BIOLOGICAL-ACTIVITY ; MITOTIC ARREST ; BREAST-CANCER ; CELL-LINES ; BINDING ; INHIBITORS ; PROTEINS ; COLCHICINE |
| 资助项目 | National Natural Science Foundation of China[90813009] ; National Natural Science Foundation of China[30873142] ; State Key Laboratory of Drug Research[00000000] |
| WOS研究方向 | Oncology |
| 语种 | 英语 |
| WOS记录号 | WOS:000298531900006 |
| 出版者 | ELSEVIER IRELAND LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278289]  |
| 专题 | 药理学第一研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Lou, Liguang |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhao, Hongbing,Quan, Haitian,Xie, Chengying,et al. YHHU0895, a novel synthetic small-molecule microtubule-destabilizing agent, effectively overcomes P-glycoprotein-mediated tumor multidrug resistance[J]. CANCER LETTERS,2012,314(1):54-62. |
| APA | Zhao, Hongbing.,Quan, Haitian.,Xie, Chengying.,Xu, Yongping.,Xie, Fuchun.,...&Lou, Liguang.(2012).YHHU0895, a novel synthetic small-molecule microtubule-destabilizing agent, effectively overcomes P-glycoprotein-mediated tumor multidrug resistance.CANCER LETTERS,314(1),54-62. |
| MLA | Zhao, Hongbing,et al."YHHU0895, a novel synthetic small-molecule microtubule-destabilizing agent, effectively overcomes P-glycoprotein-mediated tumor multidrug resistance".CANCER LETTERS 314.1(2012):54-62. |
入库方式： OAI收割
来源：上海药物研究所
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