1uou

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{{Seed}}
 
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[[Image:1uou.png|left|200px]]
 
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==Crystal structure of human thymidine phosphorylase in complex with a small molecule inhibitor==
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The line below this paragraph, containing "STRUCTURE_1uou", creates the "Structure Box" on the page.
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<StructureSection load='1uou' size='340' side='right'caption='[[1uou]], [[Resolution|resolution]] 2.11&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'>[[1uou]] is a 1 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=1UOU OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1UOU 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]] 2.11&#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=CMU:5-CHLORO-6-(1-(2-IMINOPYRROLIDINYL)+METHYL)+URACIL'>CMU</scene></td></tr>
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{{STRUCTURE_1uou| PDB=1uou | 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=1uou FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1uou OCA], [https://pdbe.org/1uou PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1uou RCSB], [https://www.ebi.ac.uk/pdbsum/1uou PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1uou ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[https://www.uniprot.org/uniprot/TYPH_HUMAN TYPH_HUMAN] Mitochondrial neurogastrointestinal encephalomyopathy. The disease is caused by mutations affecting the gene represented in this entry.<ref>PMID:9924029</ref> <ref>PMID:12177387</ref>
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== Function ==
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[https://www.uniprot.org/uniprot/TYPH_HUMAN TYPH_HUMAN] May have a role in maintaining the integrity of the blood vessels. Has growth promoting activity on endothelial cells, angiogenic activity in vivo and chemotactic activity on endothelial cells in vitro.<ref>PMID:1590793</ref> Catalyzes the reversible phosphorolysis of thymidine. The produced molecules are then utilized as carbon and energy sources or in the rescue of pyrimidine bases for nucleotide synthesis.<ref>PMID:1590793</ref>
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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/uo/1uou_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.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=1uou 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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Human thymidine phosphorylase (HTP), also known as platelet-derived endothelial cell growth factor (PD-ECGF), is overexpressed in certain solid tumors where it is linked to poor prognosis. HTP expression is utilized for certain chemotherapeutic strategies and is also thought to play a role in tumor angiogenesis. We determined the structure of HTP bound to the small molecule inhibitor 5-chloro-6-[1-(2-iminopyrrolidinyl) methyl] uracil hydrochloride (TPI). The inhibitor appears to mimic the substrate transition state, which may help explain the potency of this inhibitor and the catalytic mechanism of pyrimidine nucleotide phosphorylases (PYNPs). Further, we have confirmed the validity of the HTP structure as a template for structure-based drug design by predicting binding affinities for TPI and other known HTP inhibitors using in silico docking techniques. This work provides the first structural insight into the binding mode of any inhibitor to this important drug target and forms the basis for designing novel inhibitors for use in anticancer therapy.
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===CRYSTAL STRUCTURE OF HUMAN THYMIDINE PHOSPHORYLASE IN COMPLEX WITH A SMALL MOLECULE INHIBITOR===
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Crystal structure of human thymidine phosphorylase in complex with a small molecule inhibitor.,Norman RA, Barry ST, Bate M, Breed J, Colls JG, Ernill RJ, Luke RW, Minshull CA, McAlister MS, McCall EJ, McMiken HH, Paterson DS, Timms D, Tucker JA, Pauptit RA Structure. 2004 Jan;12(1):75-84. PMID:14725767<ref>PMID:14725767</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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The line below this paragraph, {{ABSTRACT_PUBMED_14725767}}, adds the Publication Abstract to the page
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<div class="pdbe-citations 1uou" style="background-color:#fffaf0;"></div>
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(as it appears on PubMed at http://www.pubmed.gov), where 14725767 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_14725767}}
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__TOC__
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</StructureSection>
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==About this Structure==
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1UOU is a 1 chain 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=1UOU OCA].
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==Reference==
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<ref group="xtra">PMID:14725767</ref><references group="xtra"/>
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Thymidine phosphorylase]]
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[[Category: Large Structures]]
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[[Category: Barry, S T.]]
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[[Category: Barry ST]]
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[[Category: Bate, M.]]
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[[Category: Bate M]]
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[[Category: Breed, J.]]
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[[Category: Breed J]]
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[[Category: Colls, J G.]]
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[[Category: Colls JG]]
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[[Category: Ernill, R J.]]
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[[Category: Ernill RJ]]
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[[Category: Luke, R W.A.]]
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[[Category: Luke RWA]]
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[[Category: Mcalister, M S.B.]]
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[[Category: McAlister MSB]]
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[[Category: Mccall, E J.]]
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[[Category: McCall EJ]]
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[[Category: Mcmiken, H H.J.]]
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[[Category: McMiken HHJ]]
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[[Category: Minshull, C A.]]
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[[Category: Minshull CA]]
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[[Category: Norman, R A.]]
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[[Category: Norman RA]]
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[[Category: Paterson, D S.]]
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[[Category: Paterson DS]]
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[[Category: Pauptit, R A.]]
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[[Category: Pauptit RA]]
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[[Category: Timms, D.]]
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[[Category: Timms D]]
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[[Category: Tucker, J A.]]
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[[Category: Tucker JA]]
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[[Category: Angiogenesis]]
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[[Category: Chemotaxis]]
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[[Category: Glycosyltransferase]]
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[[Category: Phosphorylase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Feb 18 00:49:29 2009''
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Current revision

Crystal structure of human thymidine phosphorylase in complex with a small molecule inhibitor

PDB ID 1uou

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