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4lva
From Proteopedia
(Difference between revisions)
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==Fragment-based Identification of Amides Derived From trans-2-(Pyridin-3-yl)cyclopropanecarboxylic Acid as Potent Inhibitors of Human Nicotinamide Phosphoribosyltransferase (NAMPT)== | ==Fragment-based Identification of Amides Derived From trans-2-(Pyridin-3-yl)cyclopropanecarboxylic Acid as Potent Inhibitors of Human Nicotinamide Phosphoribosyltransferase (NAMPT)== | ||
<StructureSection load='4lva' size='340' side='right' caption='[[4lva]], [[Resolution|resolution]] 1.55Å' scene=''> | <StructureSection load='4lva' size='340' side='right' caption='[[4lva]], [[Resolution|resolution]] 1.55Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[4lva]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/ | + | <table><tr><td colspan='2'>[[4lva]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4LVA OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4LVA FirstGlance]. <br> |
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=20M:N-(4-{[4-(PYRROLIDIN-1-YL)PIPERIDIN-1-YL]SULFONYL}BENZYL)-2H-PYRIDO[4,3-E][1,2,4]THIADIAZIN-3-AMINE+1,1-DIOXIDE'>20M</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=20M:N-(4-{[4-(PYRROLIDIN-1-YL)PIPERIDIN-1-YL]SULFONYL}BENZYL)-2H-PYRIDO[4,3-E][1,2,4]THIADIAZIN-3-AMINE+1,1-DIOXIDE'>20M</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene></td></tr> | ||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4lv9|4lv9]], [[4lvb|4lvb]], [[4lvd|4lvd]], [[4lvf|4lvf]], [[4lvg|4lvg]], [[4m6p|4m6p]], [[4m6q|4m6q]]</td></tr> | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4lv9|4lv9]], [[4lvb|4lvb]], [[4lvd|4lvd]], [[4lvf|4lvf]], [[4lvg|4lvg]], [[4m6p|4m6p]], [[4m6q|4m6q]]</td></tr> | ||
| - | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">NAMPT, PBEF, PBEF1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 | + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">NAMPT, PBEF, PBEF1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr> |
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Nicotinamide_phosphoribosyltransferase Nicotinamide phosphoribosyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.2.12 2.4.2.12] </span></td></tr> | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Nicotinamide_phosphoribosyltransferase Nicotinamide phosphoribosyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.2.12 2.4.2.12] </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=4lva FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4lva OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4lva RCSB], [http://www.ebi.ac.uk/pdbsum/4lva PDBsum]</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=4lva FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4lva OCA], [http://pdbe.org/4lva PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4lva RCSB], [http://www.ebi.ac.uk/pdbsum/4lva PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4lva ProSAT]</span></td></tr> |
</table> | </table> | ||
== Function == | == Function == | ||
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
</div> | </div> | ||
| + | <div class="pdbe-citations 4lva" style="background-color:#fffaf0;"></div> | ||
==See Also== | ==See Also== | ||
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__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: | + | [[Category: Human]] |
[[Category: Nicotinamide phosphoribosyltransferase]] | [[Category: Nicotinamide phosphoribosyltransferase]] | ||
[[Category: Bravo, B]] | [[Category: Bravo, B]] | ||
Revision as of 05:17, 5 August 2016
Fragment-based Identification of Amides Derived From trans-2-(Pyridin-3-yl)cyclopropanecarboxylic Acid as Potent Inhibitors of Human Nicotinamide Phosphoribosyltransferase (NAMPT)
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Categories: Human | Nicotinamide phosphoribosyltransferase | Bravo, B | Brien, T O | Dragovich, P S | Feng, Y | Giannetti, A M | Gunzner-Toste, J | Ho, Y | Hua, R | Liederer, B M | Liu, Y | Oeh, J | Sampath, D | Shen, Y | Skelton, N | Wang, C | Wang, L | Wang, W | Wu, H | Xiao, Y | Yuen, P | Zak, M | Zhao, G | Zhao, Q | Zheng, X | Transferase | Transferase-transferase inhibitor complex
