rdf:type |
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lifeskim:mentions |
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pubmed:issue |
14
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pubmed:dateCreated |
2008-7-21
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pubmed:abstractText |
Dipeptide derivatives bearing various P2 residues and pyrrolidine derivatives as P1 mimics were evaluated in order to identify lead structures for the development of DPP8 and DPP9 inhibitors. Structure-activity-relationship data obtained in this way led to the preparation of a series of alpha-aminoacyl ((2S, 4S)-4-azido-2-cyanopyrrolidines). These compounds were shown to be nanomolar DPP8/9 inhibitors with modest overall selectivity toward DPP IV and DPP II.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/DPP8 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/DPP9 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Dipeptidases,
http://linkedlifedata.com/resource/pubmed/chemical/Dipeptides,
http://linkedlifedata.com/resource/pubmed/chemical/Dipeptidyl-Peptidases and...,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Lysine,
http://linkedlifedata.com/resource/pubmed/chemical/Nitriles,
http://linkedlifedata.com/resource/pubmed/chemical/Peptides,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrrolidines
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AugustynsKoenK,
pubmed-author:BrandtIngerI,
pubmed-author:ChenXinX,
pubmed-author:De MeesterIngridI,
pubmed-author:DuboisVéroniqueV,
pubmed-author:HaemersAchielA,
pubmed-author:LambeirAnne-MarieAM,
pubmed-author:MaesMarie-BertheMB,
pubmed-author:ScharpéSimonS,
pubmed-author:SorokaAnnaA,
pubmed-author:Van GoethemSebastiaanS,
pubmed-author:Van der VekenPieterP
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pubmed:issnType |
Electronic
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pubmed:day |
15
|
pubmed:volume |
18
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pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
4154-8
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:18556199-Chemistry, Pharmaceutical,
pubmed-meshheading:18556199-Dipeptidases,
pubmed-meshheading:18556199-Dipeptides,
pubmed-meshheading:18556199-Dipeptidyl-Peptidases and Tripeptidyl-Peptidases,
pubmed-meshheading:18556199-Drug Design,
pubmed-meshheading:18556199-Enzyme Inhibitors,
pubmed-meshheading:18556199-Humans,
pubmed-meshheading:18556199-Inhibitory Concentration 50,
pubmed-meshheading:18556199-Lysine,
pubmed-meshheading:18556199-Models, Chemical,
pubmed-meshheading:18556199-Molecular Structure,
pubmed-meshheading:18556199-Nitriles,
pubmed-meshheading:18556199-Peptides,
pubmed-meshheading:18556199-Pyrrolidines,
pubmed-meshheading:18556199-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads.
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pubmed:affiliation |
Department of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B-2610 Antwerp, Belgium. pieter.vanderveken@ua.ac.be
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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