The prolyl-aminodipeptidases and their inhibitors as therapeutic targets for fibrogenic disorders

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State: Public
Version: Final published version
License: All rights reserved
Serval ID
serval:BIB_E4C54B5D3225
Type
Article: article from journal or magazin.
Publication sub-type
Review (review): journal as complete as possible of one specific subject, written based on exhaustive analyses from published work.
Collection
Publications
Institution
Title
The prolyl-aminodipeptidases and their inhibitors as therapeutic targets for fibrogenic disorders
Journal
Mini Reviews in Medicinal Chemistry
Author(s)
Juillerat-Jeanneret L., Gerber-Lemaire S.
ISSN
1389-5575
Publication state
Published
Issued date
2009
Peer-reviewed
Oui
Volume
9
Number
2
Pages
215-226
Language
english
Abstract
Many biologically active peptides are protected from general proteolytic degradation by evolutionary conserved prolines (Pro), due to conformational constraints imposed by the Pro residue. Thus the biological importance of prolyl-specific peptidases points to a high potential for drug discovery for this family of enzymes. Panels of inhibitors have been synthesized and their effects, determined in biological models, suggest the inhibition of families of enzymes with similar activities. Prolyl-specific aminodipeptidases include dipeptidyl-aminodipeptidase IV (DPP IV)/CD26, DPP8, DPP9 and fibroblast activation protease-alpha (FAP-alpha)/seprase, able to release X-Pro dipeptides from the N-terminus of peptides. DPP IV inhibitors are in clinical use for type 2 diabetes. In this review, the expression and the potential functions of prolyl-aminodipeptidases are reviewed in diseases, and the inhibitors developed for these enzymes are discussed, with a specific focus on inhibitors able to discriminate between DPP IV and fibroblast activation protease-alpha (FAPalpha)/seprase as potential leads for the treatment of fibrogenic diseases.
Keywords
Aminopeptidases, Animals, Antigens, Neoplasm, Dipeptidyl-Peptidase IV Inhibitors, Enzyme Inhibitors, Fibrosis, Humans, Serine Endopeptidases, Tumor Markers, Biological
Pubmed
Web of science
Create date
20/05/2009 18:31
Last modification date
11/06/2020 5:21
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