2ogz

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[[Image:2ogz.jpg|left|200px]]<br /><applet load="2ogz" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2ogz.jpg|left|200px]]
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caption="2ogz, resolution 2.100&Aring;" />
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'''Crystal structure of DPP-IV complexed with Lilly aryl ketone inhibitor'''<br />
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{{Structure
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|PDB= 2ogz |SIZE=350|CAPTION= <scene name='initialview01'>2ogz</scene>, resolution 2.100&Aring;
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|SITE=
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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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|ACTIVITY= [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]
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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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'''Crystal structure of DPP-IV complexed with Lilly aryl ketone inhibitor'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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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].
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2OGZ is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2OGZ OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17239592 17239592]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/17239592 17239592]
[[Category: Dipeptidyl-peptidase IV]]
[[Category: Dipeptidyl-peptidase IV]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: serine protease]]
[[Category: serine protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:18:28 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 17:59:37 2008''

Revision as of 15:59, 20 March 2008

Image:2ogz.jpg


PDB ID 2ogz

Drag the structure with the mouse to rotate
, resolution 2.100Å
Ligands:
Gene: DPP4, ADCP2, CD26 (Homo sapiens)
Activity: Dipeptidyl-peptidase IV, with EC number 3.4.14.5
Coordinates: save as pdb, mmCIF, xml



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 Thu Mar 20 17:59:37 2008

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