2gvg

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[[Image:2gvg.gif|left|200px]]<br /><applet load="2gvg" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2gvg.gif|left|200px]]
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caption="2gvg, resolution 2.2&Aring;" />
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'''Crystal Structure of human NMPRTase and its complex with NMN'''<br />
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{{Structure
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|PDB= 2gvg |SIZE=350|CAPTION= <scene name='initialview01'>2gvg</scene>, resolution 2.2&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene> and <scene name='pdbligand=NMN:BETA-NICOTINAMIDE RIBOSE MONOPHOSPHATE'>NMN</scene>
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|ACTIVITY= [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]
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|GENE= NAMPT ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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}}
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'''Crystal Structure of human NMPRTase and its complex with NMN'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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2GVG is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=PO4:'>PO4</scene> and <scene name='pdbligand=NMN:'>NMN</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GVG OCA].
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2GVG is a [[Single protein]] structure of 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=2GVG OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16783377 16783377]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/16783377 16783377]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Nicotinamide phosphoribosyltransferase]]
[[Category: Nicotinamide phosphoribosyltransferase]]
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[[Category: visfatin]]
[[Category: visfatin]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:35:49 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 17:09:36 2008''

Revision as of 15:09, 20 March 2008


PDB ID 2gvg

Drag the structure with the mouse to rotate
, resolution 2.2Å
Ligands: and
Gene: NAMPT (Homo sapiens)
Activity: Nicotinamide phosphoribosyltransferase, with EC number 2.4.2.12
Coordinates: save as pdb, mmCIF, xml



Crystal Structure of human NMPRTase and its complex with NMN


Overview

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.

About this Structure

2GVG is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

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

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