discoveryofanovelcompetitiveinhibitorofptp1bbyhighthroughputscreening
文献类型：期刊论文
| 作者 | Lei SHI; Haiping YU; Yueyang ZHOU; Junqin DU; Qiang SHEN; Jingya LI ; Jia LI
|
| 刊名 | actapharmacologicasinica
 |
| 出版日期 | 2008 |
| 卷号 | 29期号:2页码:278 |
| 关键词 | PROTEIN-TYROSINE PHOSPHATASE-1B FAO HEPATOMA-CELLS INSULIN SENSITIVITY ADIPOSE-TISSUE OVEREXPRESSION RESISTANCE OBESITY 1B PTP-1B GENE high throughput screening PTP1B insulin receptor phosphoryaltion competitive inhibitor |
| ISSN号 | 1671-4083 |
| DOI | 10.1111/j.1745-7254.2008.00737.x |
| 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. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/283079]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Lei SHI,Haiping YU,Yueyang ZHOU,et al. discoveryofanovelcompetitiveinhibitorofptp1bbyhighthroughputscreening[J]. actapharmacologicasinica,2008,29(2):278. |
| APA | Lei SHI.,Haiping YU.,Yueyang ZHOU.,Junqin DU.,Qiang SHEN.,...&Jia LI.(2008).discoveryofanovelcompetitiveinhibitorofptp1bbyhighthroughputscreening.actapharmacologicasinica,29(2),278. |
| MLA | Lei SHI,et al."discoveryofanovelcompetitiveinhibitorofptp1bbyhighthroughputscreening".actapharmacologicasinica 29.2(2008):278. |
入库方式： OAI收割
来源：上海药物研究所
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