2qtb

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{{STRUCTURE_2qtb| PDB=2qtb | SCENE= }}
{{STRUCTURE_2qtb| PDB=2qtb | SCENE= }}
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'''Human dipeptidyl peptidase iv/cd26 in complex with a 4-aryl cyclohexylalanine inhibitor'''
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===Human dipeptidyl peptidase iv/cd26 in complex with a 4-aryl cyclohexylalanine inhibitor===
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==Overview==
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A novel series of 4-arylcyclohexylalanine DPP-4 inhibitors was synthesized and tested for inhibitory activity as well as selectivity over the related proline-specific enzymes DPP-8 and DPP-9. Optimization of this series led to 28 (DPP-4 IC(50)=4.8 nM), which showed an excellent pharmacokinetic profile across several preclinical species. Evaluation of 28 in an oral glucose tolerance test demonstrated that this compound effectively reduced glucose excursion in lean mice.
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(as it appears on PubMed at http://www.pubmed.gov), where 17851076 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17851076}}
==About this Structure==
==About this Structure==
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[[Category: Transmembrane]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 15:38:41 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 15:07:08 2008''

Revision as of 12:07, 28 July 2008

Image:2qtb.png

Template:STRUCTURE 2qtb

Human dipeptidyl peptidase iv/cd26 in complex with a 4-aryl cyclohexylalanine inhibitor

Template:ABSTRACT PUBMED 17851076

About this Structure

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

Reference

4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV., Kaelin DE, Smenton AL, Eiermann GJ, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE, Duffy JL, Bioorg Med Chem Lett. 2007 Nov 1;17(21):5806-11. Epub 2007 Aug 26. PMID:17851076

Page seeded by OCA on Mon Jul 28 15:07:08 2008

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