2geb

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(New page: 200px<br /><applet load="2geb" size="350" color="white" frame="true" align="right" spinBox="true" caption="2geb, resolution 1.70&Aring;" /> '''Crystal structure of...)
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[[Image:2geb.jpg|left|200px]]<br /><applet load="2geb" size="350" color="white" frame="true" align="right" spinBox="true"
 
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caption="2geb, resolution 1.70&Aring;" />
 
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'''Crystal structure of the Thermoanaerobacter tengcongensis hypoxanthine-guanine phosphoribosyltransferase L160I mutant: insights into the inhibitor design'''<br />
 
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==Overview==
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==Crystal structure of the Thermoanaerobacter tengcongensis hypoxanthine-guanine phosphoribosyltransferase L160I mutant: insights into the inhibitor design==
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Hypoxanthine-guanine phosphoribosyltransferase (HGPRT) is a potential, target for structure-based inhibitor design for the treatment of parasitic, diseases. We created point mutants of Thermoanaerobacter tengcongensis, HGPRT and tested their activities to identify side chains that were, important for function. Mutating residues Leu160 and Lys133 substantially, diminished the activity of HGPRT, confirming their importance in, catalysis. All 11 HGPRT mutants were subject to crystallization screening., The crystal structure of one mutant, L160I, was determined at 1.7 A, resolution. Surprisingly, the active site is occupied by a peptide from, the N-terminus of a neighboring tetramer. These crystal contacts suggest, an alternate strategy for structure-based inhibitor design.
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<StructureSection load='2geb' size='340' side='right'caption='[[2geb]], [[Resolution|resolution]] 1.70&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[2geb]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Caldanaerobacter_subterraneus_subsp._tengcongensis Caldanaerobacter subterraneus subsp. tengcongensis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GEB OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2GEB FirstGlance]. <br>
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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]] 1.7&#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=CA:CALCIUM+ION'>CA</scene></td></tr>
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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=2geb FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2geb OCA], [https://pdbe.org/2geb PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2geb RCSB], [https://www.ebi.ac.uk/pdbsum/2geb PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2geb ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/Q8R7L0_CALS4 Q8R7L0_CALS4]
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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/ge/2geb_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=2geb ConSurf].
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<div style="clear:both"></div>
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==About this Structure==
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==See Also==
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2GEB is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Thermoanaerobacter_tengcongensis Thermoanaerobacter tengcongensis] with <scene name='pdbligand=CA:'>CA</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Hypoxanthine_phosphoribosyltransferase Hypoxanthine phosphoribosyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.2.8 2.4.2.8] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GEB OCA].
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*[[Phosphoribosyltransferase 3D structures|Phosphoribosyltransferase 3D structures]]
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__TOC__
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==Reference==
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</StructureSection>
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Crystal structure of Thermoanaerobacter tengcongensis hypoxanthine-guanine phosphoribosyl transferase L160I mutant--insights into inhibitor design., Chen Q, You D, Liang Y, Su X, Gu X, Luo M, Zheng X, FEBS J. 2007 Sep;274(17):4408-15. Epub 2007 Jul 27. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17662107 17662107]
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[[Category: Caldanaerobacter subterraneus subsp. tengcongensis]]
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[[Category: Hypoxanthine phosphoribosyltransferase]]
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[[Category: Large Structures]]
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[[Category: Single protein]]
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[[Category: Chen Q]]
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[[Category: Thermoanaerobacter tengcongensis]]
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[[Category: Luo M]]
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[[Category: Chen, Q.]]
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[[Category: Luo, M.]]
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[[Category: CA]]
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[[Category: hgprt]]
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[[Category: inhibitor design]]
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[[Category: mutant]]
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[[Category: selectivity]]
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[[Category: transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:40:37 2008''
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Current revision

Crystal structure of the Thermoanaerobacter tengcongensis hypoxanthine-guanine phosphoribosyltransferase L160I mutant: insights into the inhibitor design

PDB ID 2geb

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