期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 28, 期 6, 页码 1199-1204出版社
INFORMA HEALTHCARE
DOI: 10.3109/14756366.2012.723206
关键词
Protein tyrosine phosphatase 1B; inhibitors; 5,7-dihydroxyflavanone; structure-activity relationship; diabetes
资金
- National Natural Science Foundation of China [20962021, 81125023]
- National Program on Key Basic Research Project of China (973 Program) [2012CB524906]
A series of 5,7-dihydroxyflavanone derivatives were synthesized and identified as reversible and competitive protein tyrosine phosphatase (PTP) 1B inhibitors with IC50 values in the micromolar range. Compound 4k had the most potent in vitro inhibition activity against PTP1B (IC50 = 2.37 +/- 0.37 mu M) and the greatest selectivity (3.7-fold) for PTP1B relative to T-cell protein tyrosine phosphatase. Cell-based studies revealed that 4k was membrane-permeable and enhanced insulin receptor tyrosine phosphorylation in CHO/hIR cells.
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