2i3z

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[[Image:2i3z.jpg|left|200px]]
[[Image:2i3z.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2i3z |SIZE=350|CAPTION= <scene name='initialview01'>2i3z</scene>, resolution 2.900&Aring;
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The line below this paragraph, containing "STRUCTURE_2i3z", 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=LIR:2-[(3S)-3-AMINOPIPERIDIN-1-YL]-1-(2-CYANOBENZYL)-5-METHYL-4,6-DIOXO-3,4,5,6-TETRAHYDROPYRROLO[3,4-D]IMIDAZOL-1-IUM'>LIR</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=
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-->
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|DOMAIN=
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{{STRUCTURE_2i3z| PDB=2i3z | SCENE= }}
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|RELATEDENTRY=[[2gbi|2GBI]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2i3z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2i3z OCA], [http://www.ebi.ac.uk/pdbsum/2i3z PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2i3z RCSB]</span>
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}}
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'''rat DPP-IV with xanthine mimetic inhibitor #7'''
'''rat DPP-IV with xanthine mimetic inhibitor #7'''
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[[Category: VonGeldern, T W.]]
[[Category: VonGeldern, T W.]]
[[Category: Winn, M.]]
[[Category: Winn, M.]]
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[[Category: enzyme]]
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[[Category: Enzyme]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: peptidase]]
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[[Category: Peptidase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 07:02:24 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:39:21 2008''
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Revision as of 04:02, 4 May 2008

Template:STRUCTURE 2i3z

rat DPP-IV with xanthine mimetic inhibitor #7


Overview

A series of xanthine mimetics containing 5,5 and 5,6 heterocycle fused imidazoles were synthesized as dipeptidyl peptidase IV inhibitors. Compound 7 is potent (h-DPPIV K(i)=2nM) and exhibits excellent selectivity and no species specificity against rat and human enzymes. The X-ray structure confirms that the binding mode of 7 to rat DPPIV is similar to the parent xanthines.

About this Structure

2I3Z is a Single protein structure of sequence from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors., Kurukulasuriya R, Rohde JJ, Szczepankiewicz BG, Basha F, Lai C, Jae HS, Winn M, Stewart KD, Longenecker KL, Lubben TW, Ballaron SJ, Sham HL, von Geldern TW, Bioorg Med Chem Lett. 2006 Dec 15;16(24):6226-30. Epub 2006 Sep 28. PMID:17010607 Page seeded by OCA on Sun May 4 07:02:24 2008

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