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首页> 外文期刊>Angewandte Chemie >Models of Oxovanadium(IV)-Protein Interactions: The First Oxovanadium(IV) Complexes with Dipeptides
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Models of Oxovanadium(IV)-Protein Interactions: The First Oxovanadium(IV) Complexes with Dipeptides

机译:Oxovanadium(IV)-蛋白质相互作用的模型:首个具有二肽的Oxovanadium(IV)配合物

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Vanadium is a trace element that produces significant physiological effects; for example, vanadate inhibits ion transport ATP-ases, phosphotyrosine phosphatase etc. Arguably, the most important physiological effect is the stimulation of glucose uptakeand glucose metabolism, that is, the insulin-like properties of both vanadate and oxovanadium(IV) species. The efficacy and relative lack of toxicity of oxovanadium(IV) derivatives in animal models of diabetes makes them a potential oral therapy in human diabetes in general, and in those forms of the disease that are resistant to insulin in particular. The mode of action of oxovanadium(IV) species is still not understood. Cornman and co-workers have suggested that a possible mechanism of V~(IV)O~(2+)action is the inhibition of protein tyrosine phos-phatases (PTPascs) by binding thiolate sulfur to V~(IV)O~(2+). In addition. Sapert
机译:钒是一种微量元素,可产生显着的生理作用。例如,钒酸盐抑制离子转运ATP酶,磷酸酪氨酸磷酸酶等。可以说,最重要的生理作用是刺激葡萄糖吸收和葡萄糖代谢,即钒酸盐和氧钒(IV)物种的胰岛素样特性。在糖尿病动物模型中,氧钒(IV)衍生物的功效和相对缺乏毒性使它们在人类糖尿病中,尤其是在那些对胰岛素具有抵抗力的疾病中,成为潜在的口服疗法。氧钒(IV)物种的作用方式仍不了解。康曼及其同事提出V〜(IV)O〜(2+)作用的可能机制是通过将硫醇盐硫与V〜(IV)O〜(2)结合来抑制蛋白酪氨酸磷酸酶(PTPascs)。 +)。此外。萨珀特<!|最近,研究人员和同事报道了耶尔森牛PTPase与V〜VO_4〜(3-)的X射线晶体结构,其中钒与403-半胱氨酸残基的硫之间存在共价键。对V〜(IV)O〜(2+)作用方式和位点的阐明可以为了解胰岛素作用机理以及设计更有效的口服胰岛素替代物提供有价值的见解。

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