Dipeptidyl-peptidase IV (DPP-4) inhibitors inhibit the degradation of the incretins, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). The first available DPP-4 inhibitors are sitagliptin and vildagliptin. These compounds are orally active and have been shown to be efficacious and well tolerated. Two additional DPP-4 inhibitors are under review, and there are several others in clinical development. This article gives an overview on the mechanism of action of DPP-4 inhibitors and focuses on their development and their important physiological actions with regard to the treatment of type 2 diabetes.

中文翻译：

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二肽基肽酶-4（DPP-4）抑制剂的作用机理

二肽基肽酶IV（DPP-4）抑制剂可抑制肠降血糖素，胰高血糖素样肽1（GLP-1）和葡萄糖依赖性促胰岛素肽（GIP）的降解。第一种可用的DPP-4抑制剂是西他列汀和维格列汀。这些化合物具有口服活性，已被证明是有效的和良好的耐受性。两种其他的DPP-4抑制剂正在审查中，还有其他几种正在临床开发中。本文概述了DPP-4抑制剂的作用机理，并重点介绍了其在2型糖尿病治疗中的发展及其重要的生理作用。