Journal
ACTA PHARMACOLOGICA SINICA
Volume 29, Issue 2, Pages 278-284Publisher
ACTA PHARMACOLOGICA SINICA
DOI: 10.1111/j.1745-7254.2008.00737.x
Keywords
high throughput screening; PTP1B; insulin receptor; phosphoryaltion; competitive inhibitor
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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.
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