2ogz
From Proteopedia
(New page: 200px<br /> <applet load="2ogz" size="450" color="white" frame="true" align="right" spinBox="true" caption="2ogz, resolution 2.100Å" /> '''Crystal structure ...) |
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| - | [[Image:2ogz. | + | [[Image:2ogz.jpg|left|200px]]<br /><applet load="2ogz" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="2ogz, resolution 2.100Å" /> | caption="2ogz, resolution 2.100Å" /> | ||
'''Crystal structure of DPP-IV complexed with Lilly aryl ketone inhibitor'''<br /> | '''Crystal structure of DPP-IV complexed with Lilly aryl ketone inhibitor'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2OGZ 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 U1N as [http://en.wikipedia.org/wiki/ligand ligand]. 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:// | + | 2OGZ 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=U1N:'>U1N</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. 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=2OGZ OCA]. |
==Reference== | ==Reference== | ||
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[[Category: serine protease]] | [[Category: serine protease]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 17:40:29 2008'' |
Revision as of 15:40, 15 February 2008
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Crystal structure of DPP-IV complexed with Lilly aryl ketone inhibitor
Overview
A series of non-covalent inhibitors of the serine protease dipeptidyl, peptidase IV (DPP-IV) were found to adopt a U-shaped binding conformation, in X-ray co-crystallization studies. Remarkably, Tyr547 undergoes a 70, degrees side-chain rotation to accommodate the inhibitor and allows access, to a previously unexposed area of the protein backbone for hydrogen, bonding.
About this Structure
2OGZ is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Dipeptidyl-peptidase IV, with EC number 3.4.14.5 Full crystallographic information is available from OCA.
Reference
Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site., Sheehan SM, Mest HJ, Watson BM, Klimkowski VJ, Timm DE, Cauvin A, Parsons SH, Shi Q, Canada EJ, Wiley MR, Ruehter G, Evers B, Petersen S, Blaszczak LC, Pulley SR, Margolis BJ, Wishart GN, Renson B, Hankotius D, Mohr M, Zechel JC, Michael Kalbfleisch J, Dingess-Hammond EA, Boelke A, Weichert AG, Bioorg Med Chem Lett. 2007 Mar 15;17(6):1765-8. Epub 2006 Dec 24. PMID:17239592
Page seeded by OCA on Fri Feb 15 17:40:29 2008
Categories: Dipeptidyl-peptidase IV | Homo sapiens | Single protein | Timm, D.E. | U1N | Cd26 | Dipeptidyl peptidase iv | Dpiv | Dpp-iv | Dpp4 | Inhibitor | Serine protease
