2qoe

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[[Image:2qoe.jpg|left|200px]]
[[Image:2qoe.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2qoe |SIZE=350|CAPTION= <scene name='initialview01'>2qoe</scene>, resolution 2.30&Aring;
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The line below this paragraph, containing "STRUCTURE_2qoe", 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=448:(2R)-4-[(8R)-8-METHYL-2-(TRIFLUOROMETHYL)-5,6-DIHYDRO[1,2,4]TRIAZOLO[1,5-A]PYRAZIN-7(8H)-YL]-4-OXO-1-(2,4,5-TRIFLUOROPHENYL)BUTAN-2-AMINE'>448</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=NDG:2-(ACETYLAMINO)-2-DEOXY-A-D-GLUCOPYRANOSE'>NDG</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_2qoe| PDB=2qoe | 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=2qoe FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2qoe OCA], [http://www.ebi.ac.uk/pdbsum/2qoe PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2qoe RCSB]</span>
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}}
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'''Human Dipeptidyl Peptidase IV in complex with a Triazolopiperazine-based beta amino acid Inhibitor'''
'''Human Dipeptidyl Peptidase IV in complex with a Triazolopiperazine-based beta amino acid Inhibitor'''
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Scapin, G.]]
[[Category: Scapin, G.]]
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[[Category: alpha/beta inhibitor]]
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[[Category: Alpha/beta inhibitor]]
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[[Category: aminopeptidase]]
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[[Category: Aminopeptidase]]
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[[Category: beta-propeller,dimer]]
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[[Category: Beta-propeller,dimer]]
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[[Category: diabetes]]
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[[Category: Diabetes]]
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[[Category: glycoprotein]]
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[[Category: Glycoprotein]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: membrane]]
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[[Category: Membrane]]
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[[Category: protease]]
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[[Category: Protease]]
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[[Category: secreted]]
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[[Category: Secreted]]
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[[Category: serine protease]]
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[[Category: Serine protease]]
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[[Category: signal-anchor]]
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[[Category: Signal-anchor]]
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[[Category: transmembrane]]
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[[Category: Transmembrane]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 15:18:21 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:51:27 2008''
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Revision as of 12:18, 4 May 2008

Image:2qoe.jpg

Template:STRUCTURE 2qoe

Human Dipeptidyl Peptidase IV in complex with a Triazolopiperazine-based beta amino acid Inhibitor


Overview

Various beta-amino amides containing triazolopiperazine heterocycles have been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. These compounds display excellent oral bioavailability and good overall pharmacokinetic profiles in preclinical species. Moreover, in vivo efficacy in an oral glucose tolerance test in lean mice is demonstrated.

About this Structure

2QOE is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors., Kowalchick JE, Leiting B, Pryor KD, Marsilio F, Wu JK, He H, Lyons KA, Eiermann GJ, Petrov A, Scapin G, Patel RA, Thornberry NA, Weber AE, Kim D, Bioorg Med Chem Lett. 2007 Nov 1;17(21):5934-9. Epub 2007 Aug 23. PMID:17827003 Page seeded by OCA on Sun May 4 15:18:21 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

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