title: Novel DPP-4 inhibitors against diabetes.
abstract: DPP-4 specifically degrades the incretin hormone GLP-1 and GIP, both of which are vital modulators of blood glucose homeostasis. Attributed to its potential biological function, DPP-4 inhibition has presently represented an attractive therapeutic strategy for treating diabetes and aroused a significant interest in the pharmaceutical industry. Chemical stability, selectivity and pharmacokinetic properties have been continuously emphasized during the long journey of R&D centered on DPP-4 inhibitors. The current landscape of the development of DPP-4 inhibitors is outlined in this review, with a focus on rational drug design and structural optimization to pursue chemical stability, selectivity and favorable pharmacokinetic properties. In addition, the structure-activity relationships, based on reported DPP-4 inhibitors, will be discussed.
authors.affiliation: Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Liu
authors.forename: Yongzhou
authors.initials: Y
authors.lastname: Hu
mesh_terms: D000818:Animals; D003920:Diabetes Mellitus / Q000188:drug therapy* / Q000201:enzymology; D018819:Dipeptidyl Peptidase 4 / Q000737:chemistry / Q000378:metabolism; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D015195:Drug Design; D004355:Drug Stability; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D008958:Models, Molecular
chemical_list: D054873:Dipeptidyl-Peptidase IV Inhibitors; D007004:Hypoglycemic Agents; D018819:Dipeptidyl Peptidase 4