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4jnm
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==Discovery of Potent and Efficacious Urea-containing Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors with Reduced CYP2C9 Inhibition Properties== | ==Discovery of Potent and Efficacious Urea-containing Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors with Reduced CYP2C9 Inhibition Properties== | ||
| - | <StructureSection load='4jnm' size='340' side='right' caption='[[4jnm]], [[Resolution|resolution]] 2.20Å' scene=''> | + | <StructureSection load='4jnm' size='340' side='right'caption='[[4jnm]], [[Resolution|resolution]] 2.20Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[4jnm]] is a 2 chain structure with sequence from [ | + | <table><tr><td colspan='2'>[[4jnm]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4JNM OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4JNM FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1LJ:1-[(6-AMINOPYRIDIN-3-YL)METHYL]-3-[4-(PHENYLSULFONYL)PHENYL]UREA'>1LJ</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.2Å</td></tr> |
| - | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1LJ:1-[(6-AMINOPYRIDIN-3-YL)METHYL]-3-[4-(PHENYLSULFONYL)PHENYL]UREA'>1LJ</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene></td></tr> | |
| - | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4jnm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4jnm OCA], [https://pdbe.org/4jnm PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4jnm RCSB], [https://www.ebi.ac.uk/pdbsum/4jnm PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4jnm ProSAT]</span></td></tr> | |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | |
</table> | </table> | ||
== Function == | == Function == | ||
| - | [ | + | [https://www.uniprot.org/uniprot/NAMPT_HUMAN NAMPT_HUMAN] Catalyzes the condensation of nicotinamide with 5-phosphoribosyl-1-pyrophosphate to yield nicotinamide mononucleotide, an intermediate in the biosynthesis of NAD. It is the rate limiting component in the mammalian NAD biosynthesis pathway (By similarity). |
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==See Also== | ==See Also== | ||
| - | *[[Phosphoribosyltransferase|Phosphoribosyltransferase]] | + | *[[Phosphoribosyltransferase 3D structures|Phosphoribosyltransferase 3D structures]] |
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__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: | + | [[Category: Homo sapiens]] |
| - | [[Category: | + | [[Category: Large Structures]] |
| - | [[Category: Bair | + | [[Category: Bair KW]] |
| - | [[Category: Bauer | + | [[Category: Bauer P]] |
| - | [[Category: Baumeister | + | [[Category: Baumeister T]] |
| - | + | [[Category: Buckmelter AJ]] | |
| - | [[Category: Buckmelter | + | [[Category: Caligiuri M]] |
| - | [[Category: Caligiuri | + | [[Category: Clodfelter KH]] |
| - | [[Category: Clodfelter | + | [[Category: Dragovich PS]] |
| - | [[Category: Dragovich | + | [[Category: Fu B]] |
| - | [[Category: Fu | + | [[Category: Gunzner-Toste J]] |
| - | [[Category: Gunzner-Toste | + | [[Category: Han B]] |
| - | [[Category: Han | + | [[Category: Ho Y]] |
| - | [[Category: Ho | + | [[Category: Kley N]] |
| - | [[Category: Kley | + | [[Category: Liederer B]] |
| - | [[Category: Liederer | + | [[Category: Lin J]] |
| - | [[Category: Lin | + | [[Category: Mukadam S]] |
| - | [[Category: Mukadam | + | [[Category: O'Brien T]] |
| - | [[Category: Oh | + | [[Category: Oh A]] |
| - | [[Category: Reynolds | + | [[Category: Reynolds DJ]] |
| - | [[Category: Sharma | + | [[Category: Sharma G]] |
| - | [[Category: Skelton | + | [[Category: Skelton N]] |
| - | [[Category: Smith | + | [[Category: Smith CC]] |
| - | [[Category: Wang | + | [[Category: Wang W]] |
| - | [[Category: Wang | + | [[Category: Wang Z]] |
| - | [[Category: Xiao | + | [[Category: Xiao Y]] |
| - | [[Category: Yuen | + | [[Category: Yuen P]] |
| - | [[Category: Zak | + | [[Category: Zak M]] |
| - | [[Category: Zhang | + | [[Category: Zhang L]] |
| - | [[Category: Zhao | + | [[Category: Zhao G]] |
| - | [[Category: Zheng | + | [[Category: Zheng X]] |
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Current revision
Discovery of Potent and Efficacious Urea-containing Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors with Reduced CYP2C9 Inhibition Properties
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Categories: Homo sapiens | Large Structures | Bair KW | Bauer P | Baumeister T | Buckmelter AJ | Caligiuri M | Clodfelter KH | Dragovich PS | Fu B | Gunzner-Toste J | Han B | Ho Y | Kley N | Liederer B | Lin J | Mukadam S | O'Brien T | Oh A | Reynolds DJ | Sharma G | Skelton N | Smith CC | Wang W | Wang Z | Xiao Y | Yuen P | Zak M | Zhang L | Zhao G | Zheng X
