1rwq

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[[Image:1rwq.jpg|left|200px]]
[[Image:1rwq.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1rwq |SIZE=350|CAPTION= <scene name='initialview01'>1rwq</scene>, resolution 2.20&Aring;
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The line below this paragraph, containing "STRUCTURE_1rwq", 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=5AP:5-(AMINOMETHYL)-6-(2,4-DICHLOROPHENYL)-2-(3,5-DIMETHOXYPHENYL)PYRIMIDIN-4-AMINE'>5AP</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</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_1rwq| PDB=1rwq | SCENE= }}
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|RELATEDENTRY=[[1nu6|1NU6]], [[1nu8|1NU8]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1rwq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1rwq OCA], [http://www.ebi.ac.uk/pdbsum/1rwq PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1rwq RCSB]</span>
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}}
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'''Human Dipeptidyl peptidase IV in complex with 5-aminomethyl-6-(2,4-dichloro-phenyl)-2-(3,5-dimethoxy-phenyl)-pyrimidin-4-ylamine'''
'''Human Dipeptidyl peptidase IV in complex with 5-aminomethyl-6-(2,4-dichloro-phenyl)-2-(3,5-dimethoxy-phenyl)-pyrimidin-4-ylamine'''
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[[Category: Stihle, M.]]
[[Category: Stihle, M.]]
[[Category: Thoma, R.]]
[[Category: Thoma, R.]]
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[[Category: adenosine binding]]
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[[Category: Adenosine binding]]
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[[Category: complex structure]]
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[[Category: Complex structure]]
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[[Category: dipeptidyl peptidase iv]]
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[[Category: Dipeptidyl peptidase iv]]
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[[Category: drug design]]
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[[Category: Drug design]]
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[[Category: exopeptidase]]
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[[Category: Exopeptidase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 07:59:54 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:34:01 2008''
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Revision as of 04:59, 3 May 2008

Image:1rwq.jpg

Template:STRUCTURE 1rwq

Human Dipeptidyl peptidase IV in complex with 5-aminomethyl-6-(2,4-dichloro-phenyl)-2-(3,5-dimethoxy-phenyl)-pyrimidin-4-ylamine


Overview

The influence of aromatic substitution on a newly discovered class of inhibitors of dipeptidyl peptidase IV was investigated. A 10(5)-fold increase in potency was achieved by the optimization of aromatic substituents in a parallel chemistry program. The observed SAR could be explained by an X-ray structure of the protein-ligand complex.

About this Structure

1RWQ is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents., Peters JU, Weber S, Kritter S, Weiss P, Wallier A, Boehringer M, Hennig M, Kuhn B, Loeffler BM, Bioorg Med Chem Lett. 2004 Mar 22;14(6):1491-3. PMID:15006388 Page seeded by OCA on Sat May 3 07:59:54 2008

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OCA

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