首页> 外文期刊>Biotechnology Letters >Development of an automated protein-tyrosine phosphatase 1B inhibition assay and the screening of putative insulin-enhancing vanadium(IV) and zinc(II) complexes
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Development of an automated protein-tyrosine phosphatase 1B inhibition assay and the screening of putative insulin-enhancing vanadium(IV) and zinc(II) complexes

机译:一种自动蛋白 - 酪氨酸磷酸酶1B抑制测定和推定胰岛素增强钒(IV)和锌(II)复合物的筛选

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摘要

The inhibition of protein-tyrosine phosphatase 1B (PTP1B) is a potential target for treatment of type 2 diabetes. Vanadium and zinc metal coordinated complexes have insulin-enhancing activities, and while vanadium compounds inhibit PTP1B, little is known on the mode of action of zinc compounds. In this study we developed an automated PTP1B inhibition assay that allows for a rapid assessment of the PTP1B inhibition strength of candidate compounds. Synthetic vanadium(IV) and zinc(II) complexes were evaluated: IC50 values for vanadium complexes ranged from 0.06 to 0.8 muM whereas for zinc compounds, values were above 10 muM. Vanadium sulfate, a non-conjugated inorganic salt, had stronger inhibition activity than any of the conjugated metal complexes.
机译:抑制蛋白质 - 酪氨酸磷酸酶1B(PTP1B)是治疗2型糖尿病的潜在靶标。 钒和锌金属配位复合物具有胰岛素增强活性,而钒化合物抑制PTP1B,则在锌化合物的作用方式上众所周知。 在该研究中,我们开发了一种自动化的PTP1B抑制测定,其允许快速评估候选化合物的PTP1B抑制强度。 评价合成钒(IV)和锌(II)配合物:钒络合物的IC 50值范围为0.06至0.8米,而对于锌化合物,值高于10毫米。 硫酸钒,非缀合的无机盐,具有比任何共轭金属配合物更强的抑制活性。

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