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蛋白酪氨酸磷酸酶 1B 抑制剂作为抗糖尿病药物 - 简要综述。

Protein tyrosine phosphatase 1B inhibitors as antidiabetic agents - A brief review.

机构信息

Department of Pharmaceutical Technology, Meerut Institute of Engineering & Technology, Baghpat By-pass Crossing, NH-58, Delhi-Haridwar Highway, Meerut 250005, India.

Department of Chemistry, Indian Institute of Chemical Biology (CSIR), 4, Raja S.C. Mullick Road, Jadavpur, Kolkata 700032, W.B., India.

出版信息

Bioorg Chem. 2017 Feb;70:267-283. doi: 10.1016/j.bioorg.2016.12.004. Epub 2016 Dec 26.

DOI:10.1016/j.bioorg.2016.12.004
PMID:28043717
Abstract

Diabetes mellitus and obesity are one of the most common health issues spread throughout world and raised the medical attention to find the new effective agents to treat these disease state. Occurrence of the drug resistance to the insulin and leptin receptor is also challenging major issues. The molecules that can overcome this resistance problem could be effective for the treatment of both type II diabetes and obesity. Protein Tyrosine Phosphatase (PTP) has emerged as new promising targets for therapeutic purpose in recent years. Protein Tyrosine Phosphatase 1B (PTP 1B) act as a negative regulator of insulin and leptin receptor signalling pathways. Several approaches have been successfully applied to find out potent and selective inhibitors. This article reviews PTP 1B inhibitors; natural, synthetic and semi-synthetic that showed inhibition towards enzyme as a major target for the management of type II diabetes. These studies could be contributing the future development of PTP 1B inhibitors as drugs.

摘要

糖尿病和肥胖是全球最常见的健康问题之一,引起了医学界的关注,以寻找新的有效药物来治疗这些疾病。胰岛素和瘦素受体的耐药性的发生也是一个具有挑战性的主要问题。能够克服这种耐药性问题的分子可能对治疗 II 型糖尿病和肥胖症都有效。蛋白酪氨酸磷酸酶 (PTP) 近年来已成为治疗的有前途的新靶点。蛋白酪氨酸磷酸酶 1B (PTP1B) 作为胰岛素和瘦素受体信号通路的负调节剂。已经成功应用了几种方法来寻找有效的、选择性的抑制剂。本文综述了 PTP1B 抑制剂;天然、合成和半合成的抑制剂,它们作为治疗 II 型糖尿病的主要靶点,显示出对酶的抑制作用。这些研究可能为 PTP1B 抑制剂作为药物的未来发展做出贡献。

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