3nw2
From Proteopedia
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| - | [[ | + | ==Novel nanomolar Imidazopyridines as selective Nitric Oxide Synthase (iNOS) inhibitors: SAR and structural insights== |
| + | <StructureSection load='3nw2' size='340' side='right' caption='[[3nw2]], [[Resolution|resolution]] 2.80Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[3nw2]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3NW2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3NW2 FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=H4B:5,6,7,8-TETRAHYDROBIOPTERIN'>H4B</scene>, <scene name='pdbligand=HEM:PROTOPORPHYRIN+IX+CONTAINING+FE'>HEM</scene>, <scene name='pdbligand=MPW:2-[2-(4-METHOXYPYRIDIN-2-YL)ETHYL]-3H-IMIDAZO[4,5-B]PYRIDINE'>MPW</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr> | ||
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1nod|1nod]]</td></tr> | ||
| + | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Nitric-oxide_synthase Nitric-oxide synthase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.14.13.39 1.14.13.39] </span></td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3nw2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3nw2 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3nw2 RCSB], [http://www.ebi.ac.uk/pdbsum/3nw2 PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Inducible arginine oxidation and subsequent NO production by correspondent synthase (iNOS) are important cellular answers to proinflammatory signals. Prolonged NO production has been proved in higher organisms to cause stroke or septic shock. Several classes of potent NOS inhibitors have been reported, most of them targeting the arginine binding site of the oxygenase domain. Here we disclose the SAR and the rational design of potent and selective iNOS inhibitors which may be useful as anti-inflammatory drugs. | ||
| - | + | Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors: SAR and structural insights.,Gradler U, Fuchss T, Ulrich WR, Boer R, Strub A, Hesslinger C, Anezo C, Diederichs K, Zaliani A Bioorg Med Chem Lett. 2011 Jul 15;21(14):4228-32. Epub 2011 May 30. PMID:21684157<ref>PMID:21684157</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
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==See Also== | ==See Also== | ||
*[[Nitric Oxide Synthase|Nitric Oxide Synthase]] | *[[Nitric Oxide Synthase|Nitric Oxide Synthase]] | ||
| - | + | == References == | |
| - | == | + | <references/> |
| - | < | + | __TOC__ |
| + | </StructureSection> | ||
[[Category: Mus musculus]] | [[Category: Mus musculus]] | ||
[[Category: Nitric-oxide synthase]] | [[Category: Nitric-oxide synthase]] | ||
| - | [[Category: Anezo, C | + | [[Category: Anezo, C]] |
| - | [[Category: Boer, R | + | [[Category: Boer, R]] |
| - | [[Category: Diederichs, K | + | [[Category: Diederichs, K]] |
| - | [[Category: Fuchss, T | + | [[Category: Fuchss, T]] |
| - | [[Category: Graedler, U | + | [[Category: Graedler, U]] |
| - | [[Category: Hesslinger, C | + | [[Category: Hesslinger, C]] |
| - | [[Category: Strub, A | + | [[Category: Strub, A]] |
| - | [[Category: Ulrich, W R | + | [[Category: Ulrich, W R]] |
| - | [[Category: Zaliani, A | + | [[Category: Zaliani, A]] |
[[Category: Calmodulin-binding]] | [[Category: Calmodulin-binding]] | ||
[[Category: Fad]] | [[Category: Fad]] | ||
Revision as of 13:26, 9 December 2014
Novel nanomolar Imidazopyridines as selective Nitric Oxide Synthase (iNOS) inhibitors: SAR and structural insights
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