Acta pharmacologica Sinica, 2008-02, Vol.29 (2), p.278-284
2008
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- Autor(en) / Beteiligte
- Titel
- Discovery of a novel competitive inhibitor of PTP1B by high-throughput screening
- Ist Teil von
- Acta pharmacologica Sinica, 2008-02, Vol.29 (2), p.278-284
- Ort / Verlag
- London: Nature Publishing Group UK
- Erscheinungsjahr
- 2008
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 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 PTP 1B 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 PTPIB inhibitor LGH00081 offers a good start for structure modification and cellular functional activity study.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 1671-4083eISSN: 1745-7254DOI: 10.1111/j.1745-7254.2008.00737.xTitel-ID: cdi_proquest_miscellaneous_70233239
- Format
- –
- Schlagworte
- Animals, Biomedical and Life Sciences, Biomedicine, Catalysis, CHO Cells, Cricetinae, Cricetulus, Drug Evaluation, Preclinical, Enzyme Inhibitors - chemical synthesis, Enzyme Inhibitors - pharmacology, HTS, Humans, Immunology, Internal Medicine, Medical Microbiology, original-article, Pharmacology/Toxicology, Phosphorylation, Protein Tyrosine Phosphatase, Non-Receptor Type 1 - antagonists & inhibitors, Protein Tyrosine Phosphatase, Non-Receptor Type 1 - chemistry, Protein Tyrosine Phosphatase, Non-Receptor Type 1 - genetics, Tyrosine - metabolism, Vaccine, 竞争性抑制物, 胰岛素, 蛋白质酪氨酸磷酸酶