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.
Keywords: Dipeptidyl peptidase-IV inhibitors, Pharmacokinetic properties, Physico-chemical properties, SAR, Toxicological properties, Type 2 diabetes mellitus.
Current Topics in Medicinal Chemistry
Title:An Overview of Recent Dipeptidyl Peptidase-IV Inhibitors: Linking their Structure and Physico-Chemical Properties with SAR, Pharmacokinetics and Toxicity
Volume: 15 Issue: 23
Author(s): Andrija Smelcerovic, Filip Miljkovic, Ana Kolarevic, Jelena Lazarevic, Aleksandra Djordjevic, Gordana Kocic and Marko Anderluh
Affiliation:
Keywords: Dipeptidyl peptidase-IV inhibitors, Pharmacokinetic properties, Physico-chemical properties, SAR, Toxicological properties, Type 2 diabetes mellitus.
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.
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Smelcerovic Andrija, Miljkovic Filip, Kolarevic Ana, Lazarevic Jelena, Djordjevic Aleksandra, Kocic Gordana and Anderluh Marko, An Overview of Recent Dipeptidyl Peptidase-IV Inhibitors: Linking their Structure and Physico-Chemical Properties with SAR, Pharmacokinetics and Toxicity, Current Topics in Medicinal Chemistry 2015; 15 (23) . https://dx.doi.org/10.2174/1568026615666150619142731
DOI https://dx.doi.org/10.2174/1568026615666150619142731 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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