2gvj

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{{Seed}}
 
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[[Image:2gvj.png|left|200px]]
 
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==Crystal Structure of Human NMPRTase in complex with FK866==
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The line below this paragraph, containing "STRUCTURE_2gvj", creates the "Structure Box" on the page.
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<StructureSection load='2gvj' size='340' side='right'caption='[[2gvj]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[2gvj]] 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=2GVJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2GVJ FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.1&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DGB:(2E)-N-{4-[1-(BENZENECARBONYL)PIPERIDIN-4-YL]BUTYL}-3-(PYRIDIN-3-YL)PROP-2-ENAMIDE'>DGB</scene>, <scene name='pdbligand=MSE:SELENOMETHIONINE'>MSE</scene></td></tr>
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{{STRUCTURE_2gvj| PDB=2gvj | SCENE= }}
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2gvj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2gvj OCA], [https://pdbe.org/2gvj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2gvj RCSB], [https://www.ebi.ac.uk/pdbsum/2gvj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2gvj ProSAT]</span></td></tr>
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</table>
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== Function ==
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[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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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/gv/2gvj_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview03.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=2gvj ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Nicotinamide phosphoribosyltransferase (NMPRTase) has a crucial role in the salvage pathway of NAD+ biosynthesis, and a potent inhibitor of NMPRTase, FK866, can reduce cellular NAD+ levels and induce apoptosis in tumors. We have determined the crystal structures at up to 2.1-A resolution of human and murine NMPRTase, alone and in complex with the reaction product nicotinamide mononucleotide or the inhibitor FK866. The structures suggest that Asp219 is a determinant of substrate specificity of NMPRTase, which is confirmed by our mutagenesis studies. FK866 is bound in a tunnel at the interface of the NMPRTase dimer, and mutations in this binding site can abolish the inhibition by FK866. Contrary to current knowledge, the structures show that FK866 should compete directly with the nicotinamide substrate. Our structural and biochemical studies provide a starting point for the development of new anticancer agents.
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===Crystal Structure of Human NMPRTase in complex with FK866===
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Molecular basis for the inhibition of human NMPRTase, a novel target for anticancer agents.,Khan JA, Tao X, Tong L Nat Struct Mol Biol. 2006 Jul;13(7):582-8. Epub 2006 Jun 18. PMID:16783377<ref>PMID:16783377</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 2gvj" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_16783377}}, adds the Publication Abstract to the page
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*[[Phosphoribosyltransferase 3D structures|Phosphoribosyltransferase 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 16783377 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_16783377}}
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__TOC__
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</StructureSection>
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==About this Structure==
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2GVJ is a 2 chains structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GVJ OCA].
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==Reference==
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<ref group="xtra">PMID:16783377</ref><references group="xtra"/>
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Nicotinamide phosphoribosyltransferase]]
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[[Category: Large Structures]]
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[[Category: Khan, J A.]]
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[[Category: Khan JA]]
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[[Category: Tao, X.]]
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[[Category: Tao X]]
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[[Category: Tong, L.]]
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[[Category: Tong L]]
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[[Category: Cancer]]
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[[Category: Fk866]]
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[[Category: Nmprtase]]
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[[Category: Pbef]]
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[[Category: Visfatin]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Feb 16 21:06:14 2009''
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Current revision

Crystal Structure of Human NMPRTase in complex with FK866

PDB ID 2gvj

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