Centre for Bio-Separation Technology (CBST), Vellore Institute of Technology (VIT), Vellore, Tamil Nadu 632 014, India.
School of Bio Sciences and Technology (SBST), Vellore Institute of Technology (VIT), Vellore, Tamil Nadu 632 014, India.
Curr Protein Pept Sci. 2024;25(4):267-285. doi: 10.2174/0113892037287976231212104607.
Diabetes is a chronic metabolic disorder. According to the International Diabetes Federation, about 537 million people are living with diabetes. The two types of diabetes are type 1 diabetes mellitus (T1DM) and type 2 diabetes mellitus (T2DM), among which the population affected by T2DM is relatively higher. A major reason for T2DM is that insulin stimulation is hampered due to the inactivation of incretin hormones. Dipeptidyl peptidase-IV (DPP-IV) is a serine protease that is directly involved in the inactivation of incretin hormones, e.g., glucagon-like peptide-1 (GLP-1). Therefore, the inhibition of DPP-IV can be a promising method for managing T2DM, in addition to other enzyme inhibition strategies, such as inhibition of α-amylase and α -glucosidase. Currently, about 12 different gliptin drugs are available in the market that inhibit DPP-IV in a dose-dependent manner. Instead of gliptins, 'peptides' can also be employed as an alternative and promising way to inhibit DPP-IV. Peptide inhibitors of DPP-IV have been identified from various plants and animals. Chemically synthesized peptides have also been experimented for inhibiting DPP-IV. Most peptides have been analysed by biochemical assays, whereas some assays have also been reported. Molecular docking analysis has been applied to comprehend the mechanism of inhibition. In this review, certain aspects of natural as well as synthetic peptides are described that have been proven to inhibit DPP-IV.
糖尿病是一种慢性代谢紊乱。根据国际糖尿病联合会的数据,全球约有 5.37 亿人患有糖尿病。糖尿病有两种类型,分别是 1 型糖尿病(T1DM)和 2 型糖尿病(T2DM),其中 T2DM 的患者人群相对较高。T2DM 的一个主要原因是由于肠促胰岛素激素失活,导致胰岛素刺激受阻。二肽基肽酶-IV(DPP-IV)是一种丝氨酸蛋白酶,它直接参与肠促胰岛素激素的失活,例如胰高血糖素样肽-1(GLP-1)。因此,除了抑制α-淀粉酶和α-葡萄糖苷酶等其他酶抑制策略外,抑制 DPP-IV 可能是治疗 T2DM 的一种很有前途的方法。目前,市场上有大约 12 种不同的gliptin 药物以剂量依赖的方式抑制 DPP-IV。与 gliptins 不同,“肽”也可以作为抑制 DPP-IV 的替代和有前途的方法。已经从各种植物和动物中鉴定出 DPP-IV 的肽抑制剂。还对化学合成肽进行了抑制 DPP-IV 的实验。大多数肽都通过生化测定进行了分析,而一些测定方法也有报道。分子对接分析已被应用于理解抑制机制。在这篇综述中,描述了一些已经被证明可以抑制 DPP-IV 的天然和合成肽的某些方面。