2ole

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[[Image:2ole.jpg|left|200px]]
[[Image:2ole.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2ole |SIZE=350|CAPTION= <scene name='initialview01'>2ole</scene>, resolution 2.4&Aring;
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The line below this paragraph, containing "STRUCTURE_2ole", 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=KR2:(2R)-4-(2-BENZOYL-1,2-DIAZEPAN-1-YL)-4-OXO-1-(2,4,5-TRIFLUOROPHENYL)BUTAN-2-AMINE'>KR2</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= chromosome 2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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|DOMAIN=
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{{STRUCTURE_2ole| PDB=2ole | 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=2ole FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ole OCA], [http://www.ebi.ac.uk/pdbsum/2ole PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2ole RCSB]</span>
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}}
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'''Crystal Structure Of Human Dipeptidyl Peptidase IV (DPPIV) Complex With Cyclic Hydrazine Derivatives'''
'''Crystal Structure Of Human Dipeptidyl Peptidase IV (DPPIV) Complex With Cyclic Hydrazine Derivatives'''
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[[Category: Kim, S S.]]
[[Category: Kim, S S.]]
[[Category: Lee, J O.]]
[[Category: Lee, J O.]]
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[[Category: cyclic hydrazine]]
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[[Category: Cyclic hydrazine]]
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[[Category: diabetes]]
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[[Category: Diabetes]]
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[[Category: dipeptidyl peptidase iv]]
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[[Category: Dipeptidyl peptidase iv]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:09:22 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:19:31 2008''
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Revision as of 08:09, 4 May 2008

Image:2ole.jpg

Template:STRUCTURE 2ole

Crystal Structure Of Human Dipeptidyl Peptidase IV (DPPIV) Complex With Cyclic Hydrazine Derivatives


Overview

Inhibitors of dipeptidyl peptidase IV (DPP-IV) have been shown to be effective treatments for type 2 diabetes. A series of beta-aminoacyl-containing cyclic hydrazine derivatives were synthesized and evaluated as DPP-IV inhibitors. One member of this series, (R)-3-amino-1-(2-benzoyl-1,2-diazepan-1-yl)-4-(2,4,5-trifluorophenyl)butan -1-one (10f), showed potent in vitro activity, good selectivity and in vivo efficacy in mouse models. Also, the binding mode of compound 10f was determined by X-ray crystallography.

About this Structure

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

Reference

Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors., Ahn JH, Shin MS, Jun MA, Jung SH, Kang SK, Kim KR, Rhee SD, Kang NS, Kim SY, Sohn SK, Kim SG, Jin MS, Lee JO, Cheon HG, Kim SS, Bioorg Med Chem Lett. 2007 May 1;17(9):2622-8. Epub 2007 Feb 8. PMID:17331715 Page seeded by OCA on Sun May 4 11:09:22 2008

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