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蛋白酪氨酸磷酸酶1B及其抑制剂的研究进展

袁仲, 陈卓, 李乾斌, 胡高云

袁仲, 陈卓, 李乾斌, 胡高云. 蛋白酪氨酸磷酸酶1B及其抑制剂的研究进展[J]. 中国药科大学学报, 2018, 49(1): 1-9. DOI: 10.11665/j.issn.1000-5048.20180101
引用本文: 袁仲, 陈卓, 李乾斌, 胡高云. 蛋白酪氨酸磷酸酶1B及其抑制剂的研究进展[J]. 中国药科大学学报, 2018, 49(1): 1-9. DOI: 10.11665/j.issn.1000-5048.20180101
YUAN Zhong, CHEN Zhuo, LI Qianbin, HU Gaoyun. Advances in research of protein tyrosine phosphatase 1B and its inhibitors[J]. Journal of China Pharmaceutical University, 2018, 49(1): 1-9. DOI: 10.11665/j.issn.1000-5048.20180101
Citation: YUAN Zhong, CHEN Zhuo, LI Qianbin, HU Gaoyun. Advances in research of protein tyrosine phosphatase 1B and its inhibitors[J]. Journal of China Pharmaceutical University, 2018, 49(1): 1-9. DOI: 10.11665/j.issn.1000-5048.20180101

蛋白酪氨酸磷酸酶1B及其抑制剂的研究进展

基金项目: 国家自然科学基金资助项目(No.81573287)

Advances in research of protein tyrosine phosphatase 1B and its inhibitors

  • 摘要: 蛋白酪氨酸磷酸酶1B(protein tyrosine phosphatase 1B,PTP1B)作为蛋白酪氨酸磷酸酶(PTPs)中一员,在胰岛素和瘦素信号转导中发挥关键的负调控作用。最近研究表明,PTP1B与内质网(ER)应激、胰岛β细胞增殖以及胰岛素分泌有重要的关联;且与2型糖尿病(T2DM)和肥胖症的发生、发展密切相关,其靶向抑制剂已成为治疗这些代谢性疾病的研究热点。本文以PTP1B的结构特点及其与T2DM和肥胖症的关系为基础,根据结合位点将PTP1B抑制剂进行分类,并对其最新研究进展进行综述,旨在为靶向PTP1B的抗T2DM和肥胖症药物研发提供参考。
    Abstract: Protein tyrosine phosphatase 1B(PTP1B), a member of protein tyrosine phosphatases(PTPs), plays a key role in the negative regulation of insulin and leptin signalings. Recent studies showed that PTP1B had an important connection with endoplasmic reticulum(ER)stress, pancreatic beta cells proliferation and insulin secretion, and is closely related to the pathological process of type 2 diabetes mellitus(T2DM)and obesity. Therefore, PIP1B targeted inhibitors have become a research hotspot in the treatment of these metabolic diseases. Based on the structural features of PTP1B and its relationship with T2DM and obesity, PTP1B inhibitors were classified according to the sites of binding. Their latest research advances were reviewed in this paper, providing a reference for the development of anti-T2DM and anti-obesity drugs targeting PTP1B.
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出版历程
  • 刊出日期:  2018-02-24

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