Inhibitors of proline-specific dipeptidyl peptidases: DPP IV inhibitors as a novel approach for the treatment of Type 2 diabetes
- 30 September 2005
- journal article
- Published by Taylor & Francis in Expert Opinion on Therapeutic Patents
- Vol. 15 (10) , 1387-1407
- https://doi.org/10.1517/13543776.15.10.1387
Abstract
Dipeptidyl peptidase IV (DPP IV) is a validated target for the treatment of Type 2 diabetes, with several inhibitors currently in Phase III clinical trials. This review will mainly focus on DPP IV inhibitors that were published in scientific literature and patents after 2002. Medicinal chemistry aspects of several classes of inhibitors are described with respect to inhibitory potency, selectivity over DPP8, DPP9, FAPα and DPP II, stability and ADME/Tox issues. Although the main part of this review is on potent and selective DPP IV inhibitors, selective inhibitors for the related proline-specific dipeptidyl peptidases will be described.Keywords
This publication has 77 references indexed in Scilit:
- 1-((S)-γ-Substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitorsBioorganic & Medicinal Chemistry Letters, 2005
- METABOLIC ACTIVATION OF FLUOROPYRROLIDINE DIPEPTIDYL PEPTIDASE-IV INHIBITORS BY RAT LIVER MICROSOMESDrug Metabolism and Disposition, 2005
- Purification, identification and characterisation of seprase from bovine serumThe International Journal of Biochemistry & Cell Biology, 2004
- Inhibitors of dipeptidyl peptidase IV: a novel approach for the prevention and treatment of Type 2 diabetes?Expert Opinion on Investigational Drugs, 2004
- Aminomethylpyridines as DPP-IV inhibitorsBioorganic & Medicinal Chemistry Letters, 2004
- FAPα, a surface peptidase expressed during wound healing, is a tumor suppressorOncogene, 2004
- Seprase Promotes Rapid Tumor Growth and Increased Microvessel Density in a Mouse Model of Human Breast CancerCancer Research, 2004
- Aminomethylpyrimidines as novel DPP-IV inhibitors: A 105-fold activity increase by optimization of aromatic substituentsBioorganic & Medicinal Chemistry Letters, 2004
- Heterocycle Fused Cyclohexyl-glycine Derivatives as Novel Dipeptidyl Peptidase-IV InhibitorsHETEROCYCLES, 2004
- Dipeptidyl-Peptidase IV from Bench to Bedside: An Update on Structural Properties, Functions, and Clinical Aspects of the Enzyme DPP IVCritical Reviews in Clinical Laboratory Sciences, 2003