2oph: Difference between revisions

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[[Image:2oph.jpg|left|200px]]
{{Seed}}
[[Image:2oph.png|left|200px]]


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{{STRUCTURE_2oph|  PDB=2oph  |  SCENE=  }}  
{{STRUCTURE_2oph|  PDB=2oph  |  SCENE=  }}  


'''Human dipeptidyl peptidase IV in complex with an alpha amino acid inhibitor'''
===Human dipeptidyl peptidase IV in complex with an alpha amino acid inhibitor===




==Overview==
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A novel series of 4-aminophenylalanine and 4-aminocyclohexylalanine derivatives were designed and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4). The phenylalanine series afforded compounds such as 10 that were potent and selective (DPP-4, IC(50)=28nM), but exhibited limited oral bioavailability. The corresponding cyclohexylalanine derivatives such as 25 afforded improved PK exposure and efficacy in a murine OGTT experiment. The X-ray crystal structure of 25 bound to the DPP-4 active site is presented.
The line below this paragraph, {{ABSTRACT_PUBMED_17350841}}, adds the Publication Abstract to the page
(as it appears on PubMed at http://www.pubmed.gov), where 17350841 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17350841}}


==About this Structure==
==About this Structure==
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[[Category: Selective inhibitor]]
[[Category: Selective inhibitor]]
[[Category: Type 2 diabetes]]
[[Category: Type 2 diabetes]]
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