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

   
@article{APS4280,
	author = {Lei Shi and Hai-ping Yu and Yue-yang Zhou and Jun-qin Du and Qiang Shen and Jing-ya Li and Jia Li},
	title = {Discovery of a novel competitive inhibitor of PTP1B by high-throughput screening},
	journal = {Acta Pharmacologica Sinica},
	volume = {29},
	number = {2},
	year = {2016},
	keywords = {},
	abstract = {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.},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/4280}
}