2iiv: Difference between revisions

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[[Image:2iiv.gif|left|200px]]
{{Seed}}
[[Image:2iiv.png|left|200px]]


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{{STRUCTURE_2iiv|  PDB=2iiv  |  SCENE=  }}  
{{STRUCTURE_2iiv|  PDB=2iiv  |  SCENE=  }}  


'''Human dipeptidyl peptidase 4 in complex with a diazepan-2-one inhibitor'''
===Human dipeptidyl peptidase 4 in complex with a diazepan-2-one inhibitor===




==Overview==
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Replacement of the triazolopiperazine ring of sitagliptin (DPP-4 IC(50)=18nM) with 3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one gave dipeptidyl peptidase IV (DPP-4) inhibitor 1 which is potent (DPP-4 IC(50)=2.6nM), selective, and efficacious in an oral glucose tolerance test in mice. It was selected for extensive preclinical development as a potential back-up candidate to sitagliptin.
The line below this paragraph, {{ABSTRACT_PUBMED_17055272}}, adds the Publication Abstract to the page
(as it appears on PubMed at http://www.pubmed.gov), where 17055272 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17055272}}


==About this Structure==
==About this Structure==
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[[Category: Dimer]]
[[Category: Dimer]]
[[Category: Hydrolase]]
[[Category: Hydrolase]]
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