2ogz

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[[Image:2ogz.jpg|left|200px]]
[[Image:2ogz.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2ogz |SIZE=350|CAPTION= <scene name='initialview01'>2ogz</scene>, resolution 2.100&Aring;
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The line below this paragraph, containing "STRUCTURE_2ogz", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=U1N:4-[(3R)-3-{[2-(4-FLUOROPHENYL)-2-OXOETHYL]AMINO}BUTYL]BENZAMIDE'>U1N</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[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] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= DPP4, ADCP2, CD26 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2ogz| PDB=2ogz | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2ogz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ogz OCA], [http://www.ebi.ac.uk/pdbsum/2ogz PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2ogz RCSB]</span>
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}}
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'''Crystal structure of DPP-IV complexed with Lilly aryl ketone inhibitor'''
'''Crystal structure of DPP-IV complexed with Lilly aryl ketone inhibitor'''
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Timm, D E.]]
[[Category: Timm, D E.]]
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[[Category: cd26]]
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[[Category: Cd26]]
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[[Category: dipeptidyl peptidase iv]]
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[[Category: Dipeptidyl peptidase iv]]
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[[Category: dpiv]]
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[[Category: Dpiv]]
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[[Category: dpp-iv]]
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[[Category: Dpp-iv]]
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[[Category: dpp4]]
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[[Category: Dpp4]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: serine protease]]
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[[Category: Serine protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 10:53:46 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:17:43 2008''
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Revision as of 07:53, 4 May 2008

Image:2ogz.jpg

Template:STRUCTURE 2ogz

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. 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 Sun May 4 10:53:46 2008

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