國家衛生研究院 NHRI:Item 3990099045/9667

NHRI > Institute of Biotechnology and Pharmaceutical Research > Xin Chen(2002-2015) > Periodical Articles > Item 3990099045/9667

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Title:	Probing for improved selectivity with dipeptide-derived inhibitors of dipeptidyl peptidases 8 and 9: The impact of P1-variation
Authors:	Heirbaut, L;van Goethem, S;Jansen, K;de Winter, H;Lamoen, N;Joossens, J;Cheng, J;Chen, X;Lambeir, AM;de Meester, I;Augustyns, K;van der Veken, P
Contributors:	Institute of Biotechnology and Pharmaceutical Research
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.
Date:	2016-03
Relation:	MedChemComm. 2016 Mar;7(3):433-438.
Link to:	http://dx.doi.org/10.1039/c5md00454c
Cited Times(WOS):	https://www.webofscience.com/wos/woscc/full-record/WOS:000372218200005
Cited Times(Scopus):	http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84961841975
Appears in Collections:	[Xin Chen(2002-2015)] Periodical Articles

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