Department of Medicine, Section of Diabetes and Metabolic Diseases, University of Padova, Padova, Italy.
Br J Clin Pharmacol. 2018 Aug;84(8):1686-1695. doi: 10.1111/bcp.13611. Epub 2018 Jun 3.
Patients with Type 2 diabetes have an excess risk for cardiovascular disease. One of the several approaches, included in the guidelines for the management of Type 2 diabetes, is based on dipeptidyl peptidase 4 (DPP-4; also termed CD26) inhibitors, also called gliptins. Gliptins inhibit the degradation of glucagon-like peptide-1 (GLP-1): this effect is associated with increased circulating insulin-to-glucagon ratio, and a consequent reduction of HbA1c. In addition to incretin hormones, there are several proteins that may be affected by DPP-4 and its inhibition: among these some are relevant for the cardiovascular system homeostasis such as SDF-1α and its receptor CXCR4, brain natriuretic peptides, neuropeptide Y and peptide YY. In this review, we will discuss the pathophysiological relevance of gliptin pleiotropism and its translational potential.
2 型糖尿病患者患心血管疾病的风险过高。几种方法之一,包括 2 型糖尿病管理指南,基于二肽基肽酶 4(DPP-4;也称为 CD26)抑制剂,也称为gliptins。Gliptins 抑制胰高血糖素样肽-1(GLP-1)的降解:这种作用与循环胰岛素与胰高血糖素比值增加有关,从而导致 HbA1c 降低。除了肠降血糖素之外,还有几种可能受 DPP-4 及其抑制影响的蛋白质:其中一些与心血管系统稳态有关,例如 SDF-1α及其受体 CXCR4、脑利钠肽、神经肽 Y 和肽 YY。在这篇综述中,我们将讨论 gliptin 多效性的病理生理学相关性及其转化潜力。