2oph

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{{STRUCTURE_2oph| PDB=2oph | SCENE= }}
{{STRUCTURE_2oph| PDB=2oph | SCENE= }}
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'''Human dipeptidyl peptidase IV in complex with an alpha amino acid inhibitor'''
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===Human dipeptidyl peptidase IV in complex with an alpha amino acid inhibitor===
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==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.
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(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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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:23:33 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 04:12:10 2008''

Revision as of 01:12, 28 July 2008

Template:STRUCTURE 2oph

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

Template:ABSTRACT PUBMED 17350841

About this Structure

2OPH is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV., Duffy JL, Kirk BA, Wang L, Eiermann GJ, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE, Bioorg Med Chem Lett. 2007 May 15;17(10):2879-85. Epub 2007 Feb 25. PMID:17350841

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