2qt9
From Proteopedia
(New page: 200px<br /> <applet load="2qt9" size="450" color="white" frame="true" align="right" spinBox="true" caption="2qt9, resolution 2.100Å" /> '''Human dipeptidyl p...) |
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| - | [[Image:2qt9. | + | [[Image:2qt9.jpg|left|200px]]<br /><applet load="2qt9" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2qt9" size=" | + | |
caption="2qt9, resolution 2.100Å" /> | caption="2qt9, resolution 2.100Å" /> | ||
'''Human dipeptidyl peptidase iv/cd26 in complex with a 4-aryl cyclohexylalanine inhibitor'''<br /> | '''Human dipeptidyl peptidase iv/cd26 in complex with a 4-aryl cyclohexylalanine inhibitor'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2QT9 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with NAG, NA and 524 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Dipeptidyl-peptidase_IV Dipeptidyl-peptidase IV], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.14.5 3.4.14.5] Full crystallographic information is available from [http:// | + | 2QT9 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=NAG:'>NAG</scene>, <scene name='pdbligand=NA:'>NA</scene> and <scene name='pdbligand=524:'>524</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Dipeptidyl-peptidase_IV Dipeptidyl-peptidase IV], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.14.5 3.4.14.5] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2QT9 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: transmembrane]] | [[Category: transmembrane]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:23:56 2008'' |
Revision as of 10:23, 23 January 2008
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Human dipeptidyl peptidase iv/cd26 in complex with a 4-aryl cyclohexylalanine inhibitor
Overview
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.
About this Structure
2QT9 is a Single protein structure of sequence from Homo sapiens with , and as ligands. Active as Dipeptidyl-peptidase IV, with EC number 3.4.14.5 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 Wed Jan 23 12:23:56 2008
Categories: Dipeptidyl-peptidase IV | Homo sapiens | Single protein | Scapin, G. | 524 | NA | NAG | Alpha/beta | Aminopeptidase | Beta-propeller | Dimer | Glycoprotein | Hydrolase | Membrane | Protease | Secreted | Serine protease | Signal-anchor | Transmembrane
