Discovery of a novel competitive inhibitor of PTP1B by high-throughput screening
文献类型：期刊论文
| 作者 | Shi, Lei; Yu, Hai-ping; Zhou, Yue-yang; Du, Jun-qin; Shen, Qiang; Li, Jing-ya ; Li, Jia
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2008-02 |
| 卷号 | 29期号:2页码:278-284 |
| 关键词 | high throughput screening PTP1B insulin receptor phosphoryaltion competitive inhibitor |
| ISSN号 | 1671-4083 |
| DOI | 10.1111/j.1745-7254.2008.00737.x |
| 文献子类 | Article |
| 英文摘要 | Aim: The aim of the present study was to discover novel protein tyrosine phosphatase 1B (PTP1B) inhibitors. We expressed and purified the human PTP1B catalytic domain and set up a molecular level high-throughput screening (HTS) assay to screen a set of 48 000 pure compounds. Results: HTS was finished with an averaged Z' factor of 0.63, and LGH00081, a competitive inhibitor of PTP1B with novel structure and relatively good selectivity for receptor-type protein tyrosine phosphatases, was identified. Conclusion: We established a molecular level assay which is useful for the screening of PTP1B inhibitors with therapeutic potential. The novel competitive PTP1B inhibitor LGH00081 offers a good start for structure modification and cellular functional activity study. |
| WOS关键词 | PROTEIN-TYROSINE PHOSPHATASE-1B ; FAO HEPATOMA-CELLS ; INSULIN SENSITIVITY ; ADIPOSE-TISSUE ; OVEREXPRESSION ; RESISTANCE ; OBESITY ; 1B ; PTP-1B ; GENE |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:3249772 |
| WOS记录号 | WOS:000252805200020 |
| 出版者 | BLACKWELL PUBLISHING |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272984]  |
| 专题 | 国家新药筛选中心 药物安全性评价中心 |
| 通讯作者 | Li, Jia |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Shi, Lei,Yu, Hai-ping,Zhou, Yue-yang,et al. Discovery of a novel competitive inhibitor of PTP1B by high-throughput screening[J]. ACTA PHARMACOLOGICA SINICA,2008,29(2):278-284. |
| APA | Shi, Lei.,Yu, Hai-ping.,Zhou, Yue-yang.,Du, Jun-qin.,Shen, Qiang.,...&Li, Jia.(2008).Discovery of a novel competitive inhibitor of PTP1B by high-throughput screening.ACTA PHARMACOLOGICA SINICA,29(2),278-284. |
| MLA | Shi, Lei,et al."Discovery of a novel competitive inhibitor of PTP1B by high-throughput screening".ACTA PHARMACOLOGICA SINICA 29.2(2008):278-284. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。