Dipeptidyl peptidase-4 inhibitors: Multitarget drugs, not only antidiabetes drugs (D ipeptidyl peptidase -4抑制剂:多靶点药物,不仅仅是降糖药)

Authors

  • Yunjuan Zhao,

    1. Diabetes Center, Institute of Metabolism and Endocrinology, The Second Xiangya Hospital and Key Laboratory of Diabetes Immunology, Ministry of Education, Central South University, Changsha, China
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  • Lin Yang,

    1. Diabetes Center, Institute of Metabolism and Endocrinology, The Second Xiangya Hospital and Key Laboratory of Diabetes Immunology, Ministry of Education, Central South University, Changsha, China
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  • Zhiguang Zhou

    Corresponding author
    1. Diabetes Center, Institute of Metabolism and Endocrinology, The Second Xiangya Hospital and Key Laboratory of Diabetes Immunology, Ministry of Education, Central South University, Changsha, China
    • Correspondence

      Zhiguang Zhou, Middle Ren-Min Road No.139, Changsha, Hunan 410011, China.

      Tel: +86 731 85292154

      Fax: +86 731 85267220

      Email: zhouzg@hotmail.com

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Abstract

Dipeptidyl peptidase (DPP)-4 inhibitors are a new class of antidiabetic agents that reduce blood glucose by preventing the degradation of the endogenous incretin hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide. Protection by DPP-4 inhibitors of β-cell function has been demonstrated in patients with type 2 diabetes. Because DPP-4 is an enzyme widely expressed in humans, DPP-4 inhibitors are speculated to be multitarget agents. However, other potential therapeutic benefits of DPP-4 inhibitors remain unknown. Recently, some therapeutic effects of DPP-4 inhibitors, such as immune regulation, cardiovascular protection, and anti-inflammatory effects, have been observed. This article provides a systematic and comprehensive review of current research into the newly found effects and mechanism of action of DPP-4 inhibitors in a therapeutic context.

摘要

二肽基肽酶-4(Dipeptidyl peptidase-4,DPP-4)抑制剂是一种新型降糖药物,主要通过抑制内源性肠促胰岛素-胰高血糖素样肽-1和葡萄糖依赖性促胰岛素多肽的降解而起到降血糖的作用。许多研究已证实DPP-4抑制剂对2型糖尿病患者的胰岛β细胞具有保护作用。DPP-4是一种在体内广泛表达的酶,由此推测DPP-4抑制剂是一种多靶点的药物。然而, DPP-4抑制剂其他的潜在治疗作用目前仍不甚清楚。最近一些研究已经观察到DPP-4抑制剂具有免疫调节、心血管保护和抗炎等治疗作用。本文就最近新发现的DPP-4抑制剂的作用及机制做系统性综述。

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