Discovery of a novel competitive inhibitor of PTP1B by high-throughput screening

doi:10.1111/j.1745-7254.2008.00737.x

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	Discovery of a novel competitive inhibitor of PTP1B by high-throughput screening
	Shi, Lei; Yu, Hai-ping; Zhou, Yue-yang; Du, Jun-qin; Shen, Qiang; Li, Jing-ya; Li, Jia
刊名	ACTA PHARMACOLOGICA SINICA
	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
出版者	BLACKWELL PUBLISHING
WOS记录号	WOS:000252805200020
内容类型	期刊论文
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.