2oqi

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[[Image:2oqi.gif|left|200px]]
[[Image:2oqi.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2oqi |SIZE=350|CAPTION= <scene name='initialview01'>2oqi</scene>, resolution 2.800&Aring;
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The line below this paragraph, containing "STRUCTURE_2oqi", 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=GGO:(4R,5R)-5-AMINO-1-[2-(1,3-BENZODIOXOL-5-YL)ETHYL]-4-(2,4,5-TRIFLUOROPHENYL)PIPERIDIN-2-ONE'>GGO</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_2oqi| PDB=2oqi | 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=2oqi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2oqi OCA], [http://www.ebi.ac.uk/pdbsum/2oqi PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2oqi RCSB]</span>
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}}
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'''Human Dipeptidyl Peptidase IV (DPP4) with Piperidinone-constrained phenethylamine'''
'''Human Dipeptidyl Peptidase IV (DPP4) with Piperidinone-constrained phenethylamine'''
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[[Category: Stewart, K D.]]
[[Category: Stewart, K D.]]
[[Category: Trevillyan, J M.]]
[[Category: Trevillyan, J M.]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: serine-peptidase]]
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[[Category: Serine-peptidase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:27:31 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:21:41 2008''
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Revision as of 08:27, 4 May 2008

Image:2oqi.gif

Template:STRUCTURE 2oqi

Human Dipeptidyl Peptidase IV (DPP4) with Piperidinone-constrained phenethylamine


Overview

Dipeptidyl peptidase IV (DPP4) inhibitors are emerging as a new class of therapeutic agents for the treatment of type 2 diabetes. They exert their beneficial effects by increasing the levels of active glucagon-like peptide-1 and glucose-dependent insulinotropic peptide, which are two important incretins for glucose homeostasis. Starting from a high-throughput screening hit, we were able to identify a series of piperidinone- and piperidine-constrained phenethylamines as novel DPP4 inhibitors. Optimized compounds are potent, selective, and have good pharmacokinetic profiles.

About this Structure

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

Reference

Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors., Pei Z, Li X, von Geldern TW, Longenecker K, Pireh D, Stewart KD, Backes BJ, Lai C, Lubben TH, Ballaron SJ, Beno DW, Kempf-Grote AJ, Sham HL, Trevillyan JM, J Med Chem. 2007 Apr 19;50(8):1983-7. Epub 2007 Mar 17. PMID:17367123 Page seeded by OCA on Sun May 4 11:27:31 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

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