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蛋白酪氨酸磷酸酶-1B(PTP-1B)是胰岛素信号转导的主要负调控因子,对2型糖尿病的发生、发展有重要作用。PTP-1B通过使胰岛素受体及其底物酪氨酸去磷酸化而阻断胰岛素的信号转导。2型糖尿病患者和动物模型PTP-1B的表达水平和活性均明显提高,引起胰岛素抵抗,而PTP-1B 基因敲除鼠胰岛素敏感性却升高。因此,深入研究PTP-1B及其有效的抑制剂对于2型糖尿病的治疗具有良好的发展前景。
Protein tyrosine phosphatase-1B (PTP-1B) is a major negative regulator of insulin signaling and plays an important role in the development of type 2 diabetes mellitus. PTP-1B blocks insulin signal transduction by dephosphorylating the insulin receptor and its substrate tyrosine. The expression level and activity of PTP-1B in patients with type 2 diabetes mellitus and animal models were significantly increased, leading to insulin resistance, whereas the insulin sensitivity of PTP-1B knockout mice increased. Therefore, in-depth study of PTP-1B and its effective inhibitors for the treatment of type 2 diabetes has good prospects for development.