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Issue 3, 2016
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Probing for improved selectivity with dipeptide-derived inhibitors of dipeptidyl peptidases 8 and 9: the impact of P1-variation

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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.

Graphical abstract: Probing for improved selectivity with dipeptide-derived inhibitors of dipeptidyl peptidases 8 and 9: the impact of P1-variation

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Supplementary files

Article information


Submitted
03 Oct 2015
Accepted
18 Nov 2015
First published
19 Nov 2015

Med. Chem. Commun., 2016,7, 433-438
Article type
Research Article

Probing for improved selectivity with dipeptide-derived inhibitors of dipeptidyl peptidases 8 and 9: the impact of P1-variation

L. Heirbaut, S. van Goethem, K. Jansen, H. de Winter, N. Lamoen, J. Joossens, J. Cheng, X. Chen, A. Lambeir, I. de Meester, K. Augustyns and P. van der Veken, Med. Chem. Commun., 2016, 7, 433
DOI: 10.1039/C5MD00454C

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