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Title
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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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Author
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Abstract
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| 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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Language
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English
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Source (journal)
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MedChemComm
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Publication
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2016
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ISSN
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2040-2503
2040-2511
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DOI
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10.1039/C5MD00454C
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Volume/pages
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7
:3
(2016)
, p. 433-438
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ISI
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000372218200005
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Full text (Publisher's DOI)
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Full text (open access)
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Full text (publisher's version - intranet only)
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