Publication
Title
Probing for improved selectivity with dipeptide-derived inhibitors of dipeptidyl peptidases 8 and 9 : the impact of P1-variation
Author
Abstract
Selected pyrrolidines, 2-cyanopyrrolidines and heteroaromatic isoindoline analogues were evaluated as P1-residues in dipeptide-derived inhibitors of DPP8/9. Potency testing indicates that DPP8 or DPP9 specificity cannot be obtained with the selected set of P1- and P2-fragments. Nonetheless, the nanomolar DPP8/9 potencies and remarkable selectivities with respect to DPP IV and DPPII, makes inhibitors 4c and 4h suitable "leads" for future inhibitor optimization effort.
Language
English
Source (journal)
MedChemComm
Publication
2016
ISSN
2040-2503
2040-2511
Volume/pages
7:3(2016), p. 433-438
ISI
000372218200005
Full text (Publisher's DOI)
Full text (open access)
Full text (publisher's version - intranet only)
UAntwerpen
Faculty/Department
Research group
Publication type
Subject
Affiliation
Publications with a UAntwerp address
External links
Web of Science
Record
Identification
Creation 10.05.2016
Last edited 31.07.2017
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