2q8z

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[[Image:2q8z.jpg|left|200px]]
[[Image:2q8z.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2q8z |SIZE=350|CAPTION= <scene name='initialview01'>2q8z</scene>, resolution 1.80&Aring;
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The line below this paragraph, containing "STRUCTURE_2q8z", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:So4+Binding+Site+For+Residue+A+501'>AC1</scene>, <scene name='pdbsite=AC2:So4+Binding+Site+For+Residue+B+501'>AC2</scene>, <scene name='pdbsite=AC3:Nup+Binding+Site+For+Residue+A+401'>AC3</scene>, <scene name='pdbsite=AC4:Nup+Binding+Site+For+Residue+B+401'>AC4</scene>, <scene name='pdbsite=AC5:7pe+Binding+Site+For+Residue+A+601'>AC5</scene>, <scene name='pdbsite=AC6:Peg+Binding+Site+For+Residue+A+701'>AC6</scene> and <scene name='pdbsite=AC7:Peg+Binding+Site+For+Residue+B+701'>AC7</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=7PE:2-(2-(2-(2-(2-(2-ETHOXYETHOXY)ETHOXY)ETHOXY)ETHOXY)ETHOXY)ETHANOL'>7PE</scene>, <scene name='pdbligand=NUP:6-AMINOURIDINE+5&#39;-MONOPHOSPHATE'>NUP</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE= PF10_0225 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=36329 Plasmodium falciparum 3D7])
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-->
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|DOMAIN=
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{{STRUCTURE_2q8z| PDB=2q8z | SCENE= }}
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|RELATEDENTRY=[[2q8l|2Q8L]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2q8z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2q8z OCA], [http://www.ebi.ac.uk/pdbsum/2q8z PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2q8z RCSB]</span>
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}}
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'''Crystal structure of Plasmodium falciparum orotidine 5'-phosphate decarboxylase complexed with 6-amino-UMP'''
'''Crystal structure of Plasmodium falciparum orotidine 5'-phosphate decarboxylase complexed with 6-amino-UMP'''
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[[Category: Pai, E F.]]
[[Category: Pai, E F.]]
[[Category: 6-amino-ump]]
[[Category: 6-amino-ump]]
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[[Category: lyase]]
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[[Category: Lyase]]
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[[Category: orotidine 5'-phosphate decarboxylase]]
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[[Category: Orotidine 5'-phosphate decarboxylase]]
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[[Category: plasmodium falciparum]]
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[[Category: Plasmodium falciparum]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:33:12 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:46:24 2008''
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Revision as of 11:33, 4 May 2008

Image:2q8z.jpg

Template:STRUCTURE 2q8z

Crystal structure of Plasmodium falciparum orotidine 5'-phosphate decarboxylase complexed with 6-amino-UMP


Overview

Malaria, caused by Plasmodia parasites, has re-emerged as a major problem, imposing its fatal effects on human health, especially due to multidrug resistance. In Plasmodia, orotidine 5'-monophosphate decarboxylase (ODCase) is an essential enzyme for the de novo synthesis of uridine 5'-monophosphate. Impairing ODCase in these pathogens is a promising strategy to develop novel classes of therapeutics. Encouraged by our recent discovery that 6-iodo uridine is a potent inhibitor of P. falciparum, we investigated the structure-activity relationships of various C6 derivatives of UMP. 6-Cyano, 6-azido, 6-amino, 6-methyl, 6- N-methylamino, and 6- N, N-dimethylamino derivatives of uridine were evaluated against P. falciparum. The mononucleotides of 6-cyano, 6-azido, 6-amino, and 6-methyl uridine derivatives were studied as inhibitors of plasmodial ODCase. 6-Azidouridine 5'-monophosphate is a potent covalent inhibitor of P. falciparum ODCase. 6-Methyluridine exhibited weak antimalarial activity against P. falciparum 3D7 isolate. 6- N-Methylamino and 6- N, N-dimethylamino uridine derivatives exhibited moderate antimalarial activities.

About this Structure

2Q8Z is a Single protein structure of sequence from Plasmodium falciparum 3d7. Full crystallographic information is available from OCA.

Reference

Structure-Activity Relationships of C6-Uridine Derivatives Targeting Plasmodia Orotidine Monophosphate Decarboxylase., Bello AM, Poduch E, Liu Y, Wei L, Crandall I, Wang X, Dyanand C, Kain KC, Pai EF, Kotra LP, J Med Chem. 2008 Feb 14;51(3):439-448. Epub 2008 Jan 12. PMID:18189347 Page seeded by OCA on Sun May 4 14:33:12 2008

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