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{{STRUCTURE_4lva|  PDB=4lva  |  SCENE=  }}
===Fragment-based Identification of Amides Derived From trans-2-(Pyridin-3-yl)cyclopropanecarboxylic Acid as Potent Inhibitors of Human Nicotinamide Phosphoribosyltransferase (NAMPT)===
{{ABSTRACT_PUBMED_24021463}}


==Function==
==Fragment-based Identification of Amides Derived From trans-2-(Pyridin-3-yl)cyclopropanecarboxylic Acid as Potent Inhibitors of Human Nicotinamide Phosphoribosyltransferase (NAMPT)==
[[http://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).  
<StructureSection load='4lva' size='340' side='right'caption='[[4lva]], [[Resolution|resolution]] 1.55&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[4lva]] 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=4LVA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4LVA FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.55&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><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='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4lva FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4lva OCA], [https://pdbe.org/4lva PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4lva RCSB], [https://www.ebi.ac.uk/pdbsum/4lva PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4lva ProSAT]</span></td></tr>
</table>
== 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).


==About this Structure==
==See Also==
[[4lva]] is a 2 chain structure with sequence 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=4LVA OCA].
*[[Phosphoribosyltransferase 3D structures|Phosphoribosyltransferase 3D structures]]
 
__TOC__
==Reference==
</StructureSection>
<ref group="xtra">PMID:024021463</ref><references group="xtra"/><references/>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Nicotinamide phosphoribosyltransferase]]
[[Category: Large Structures]]
[[Category: Bravo, B.]]
[[Category: Bravo B]]
[[Category: Brien, T O.]]
[[Category: Dragovich PS]]
[[Category: Dragovich, P S.]]
[[Category: Feng Y]]
[[Category: Feng, Y.]]
[[Category: Giannetti AM]]
[[Category: Giannetti, A M.]]
[[Category: Gunzner-Toste J]]
[[Category: Gunzner-Toste, J.]]
[[Category: Ho Y]]
[[Category: Ho, Y.]]
[[Category: Hua R]]
[[Category: Hua, R.]]
[[Category: Liederer BM]]
[[Category: Liederer, B M.]]
[[Category: Liu Y]]
[[Category: Liu, Y.]]
[[Category: O'Brien T]]
[[Category: Oeh, J.]]
[[Category: Oeh J]]
[[Category: Sampath, D.]]
[[Category: Sampath D]]
[[Category: Shen, Y.]]
[[Category: Shen Y]]
[[Category: Skelton, N.]]
[[Category: Skelton N]]
[[Category: Wang, C.]]
[[Category: Wang C]]
[[Category: Wang, L.]]
[[Category: Wang L]]
[[Category: Wang, W.]]
[[Category: Wang W]]
[[Category: Wu, H.]]
[[Category: Wu H]]
[[Category: Xiao, Y.]]
[[Category: Xiao Y]]
[[Category: Yuen, P.]]
[[Category: Yuen P]]
[[Category: Zak, M.]]
[[Category: Zak M]]
[[Category: Zhao, G.]]
[[Category: Zhao G]]
[[Category: Zhao, Q.]]
[[Category: Zhao Q]]
[[Category: Zheng, X.]]
[[Category: Zheng X]]
[[Category: Transferase]]
[[Category: Transferase-transferase inhibitor complex]]

Latest revision as of 15:21, 1 March 2024

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)

Structural highlights

4lva is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 1.55Å
Ligands:, ,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

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).

See Also

4lva, resolution 1.55Å

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