title: An overview of recent dipeptidyl peptidase-IV inhibitors: linking their structure and physico-chemical properties with sar, pharmacokinetics and toxicity.
abstract: Dipeptidyl peptidase-IV (DPP-IV) (EC 3.4.14.5) is а member of the broad class of hydrolytic enzymes which is responsible for degradation of the incretin peptide hormones regulating blood glucose levels. In this article we review the literature on natural and synthetic DPP-IV inhibitors, focusing their chemical structure and mechanism of action. Further, physico-chemical, pharmacokinetic and toxicological properties of DPP-IV inhibitors are calculated and compared. On the basis of literature data we selected the DPP-IV inhibitors with IC50 values below 1 nM and discussed their possible application in therapy of type 2 diabetes mellitus.
authors.affiliation: Department of Chemistry, Faculty of Medicine, University of Nis, Bulevar Dr Zorana Djindjica 81, 18000 Nis, Serbia. a.smelcerovic@yahoo.com.
authors.forename: Andrija
authors.initials: A
authors.lastname: Smelcerovic
authors.forename: Filip
authors.initials: F
authors.lastname: Miljkovic
authors.forename: Ana
authors.initials: A
authors.lastname: Kolarevic
authors.forename: Jelena
authors.initials: J
authors.lastname: Lazarevic
authors.forename: Aleksandra
authors.initials: A
authors.lastname: Djordjevic
authors.forename: Gordana
authors.initials: G
authors.lastname: Kocic
authors.forename: Marko
authors.initials: M
authors.lastname: Anderluh
mesh_terms: D000818:Animals; D001688:Biological Products / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D001786:Blood Glucose / Q000378:metabolism; D055598:Chemical Phenomena; D003924:Diabetes Mellitus, Type 2 / Q000097:blood / Q000188:drug therapy; D018819:Dipeptidyl Peptidase 4 / Q000378:metabolism; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D007928:Lethal Dose 50; D015394:Molecular Structure; D011237:Predictive Value of Tests; D011485:Protein Binding; D013329:Structure-Activity Relationship; D013379:Substrate Specificity; D018675:Toxicity Tests
chemical_list: D001688:Biological Products; D001786:Blood Glucose; D054873:Dipeptidyl-Peptidase IV Inhibitors; D007004:Hypoglycemic Agents; D018819:Dipeptidyl Peptidase 4