Title
Probing for improved selectivity with dipeptide-derived inhibitors of dipeptidyl peptidases 8 and 9 : the impact of P1-variation Probing for improved selectivity with dipeptide-derived inhibitors of dipeptidyl peptidases 8 and 9 : the impact of P1-variation
Author
Faculty/Department
Faculty of Sciences. Biology
Faculty of Pharmaceutical, Biomedical and Veterinary Sciences. Pharmacy
Publication type
article
Publication
Subject
Chemistry
Biology
Pharmacology. Therapy
Source (journal)
MedChemComm
Volume/pages
7(2016) :3 , p. 433-438
ISSN
2040-2503
ISI
000372218200005
Carrier
E
Target language
English (eng)
Full text (Publishers DOI)
Affiliation
University of Antwerp
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.
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https://repository.uantwerpen.be/docman/iruaauth/bc4f91/133215.pdf
Full text (open access)
https://repository.uantwerpen.be/docman/irua/d89bd4/129223.pdf
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