Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates.

Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates. Research Abstract Details 

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Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates. Abstract Text:

Pieter Van der Veken,Anna Soroka,Inger Brandt,Yuan-Shou Chen,Marie-Berthe Maes,Anne-Marie Lambeir,Xin Chen,Achiel Haemers,Simon ,Koen Augustyns,Ingrid De Meester,Pieter Van der Veken,Anna Soroka,Inger Brandt,Yuan-Shou Chen,Marie-Berthe Maes,Anne-Marie Lambeir,Xin Chen,Achiel Haemers,Simon ,Koen Augustyns,Ingrid De Meester,

Dipeptide-derived compounds, bearing various P2 residues and a diaryl pyrrolidin-2-yl phosphonate at the P1 position, were evaluated as dipeptidyl peptidase 8 (DPP8) inhibitors. With these products, irreversible inhibition of DPP8 was observed. To obtain inhibitors with an improved activity and selectivity profile, a set of selected analogues containing a diaryl isoindolin-1-ylphosphonate at P1 was synthesized and evaluated. Within this latter series, compound 2e was shown to be a potent, irreversible inhibitor of DPP8, demonstrating very low affinity for DPP IV and DPP II.

Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates. Publishing Authors By Initials

P Van der Veken,A Soroka,I Brandt,YS Chen,MB Maes,AM Lambeir,X Chen,A Haemers,S ,K Augustyns,I De Meester,P Van der Veken,A Soroka,I Brandt,YS Chen,MB Maes,AM Lambeir,X Chen,A Haemers,S ,K Augustyns,I De Meester,

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Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Journal of medicinal chemistry

VOLUME: 50

Page Numbers: 5568-70

Journal Abbreviation: J. Med. Chem.

ISSN: 0022-2623

DAY: 24

MONTH: 10

YEAR: 2007

Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates. Information

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LANGUAGE: eng

NlmUniqueID: 9716531

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Grant and Affiliation Information for Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates.

AFFILIATION: Laboratory of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B-2610 Antwerp, Belgium. pieter.vanderveken@ua.ac.be

Country: United States

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MEDLINETA: J Med Chem

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