2f16

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(New page: 200px<br /><applet load="2f16" size="450" color="white" frame="true" align="right" spinBox="true" caption="2f16, resolution 2.8&Aring;" /> '''Crystal structure of ...)
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[[Image:2f16.gif|left|200px]]<br /><applet load="2f16" size="450" color="white" frame="true" align="right" spinBox="true"
 
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caption="2f16, resolution 2.8&Aring;" />
 
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'''Crystal structure of the yeast 20S proteasome in complex with bortezomib'''<br />
 
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==Overview==
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==Crystal structure of the yeast 20S proteasome in complex with bortezomib==
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The dipeptide boronic acid bortezomib, also termed VELCADE, is a, proteasome inhibitor now in use for the treatment of multiple myeloma, and, its use for the treatment of other malignancies is being explored. We, determined the crystal structure of the yeast 20S proteasome in complex, with bortezomib to establish the specificity and binding mode of, bortezomib to the proteasome's different catalytically active sites. This, structure should enable the rational design of new boronic acid, derivatives with improved affinities and specificities for individual, active subunits.
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<StructureSection load='2f16' size='340' side='right'caption='[[2f16]], [[Resolution|resolution]] 2.80&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[2f16]] is a 20 chain structure with sequence from [https://en.wikipedia.org/wiki/Saccharomyces_cerevisiae Saccharomyces cerevisiae]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2F16 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2F16 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]] 2.8&#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=BO2:N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE'>BO2</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=2f16 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2f16 OCA], [https://pdbe.org/2f16 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2f16 RCSB], [https://www.ebi.ac.uk/pdbsum/2f16 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2f16 ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/PSA2_YEAST PSA2_YEAST] The proteasome degrades poly-ubiquitinated proteins in the cytoplasm and in the nucleus. It is essential for the regulated turnover of proteins and for the removal of misfolded proteins. The proteasome is a multicatalytic proteinase complex that is characterized by its ability to cleave peptides with Arg, Phe, Tyr, Leu, and Glu adjacent to the leaving group at neutral or slightly basic pH. It has an ATP-dependent proteolytic activity.
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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/f1/2f16_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview03.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=2f16 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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The dipeptide boronic acid bortezomib, also termed VELCADE, is a proteasome inhibitor now in use for the treatment of multiple myeloma, and its use for the treatment of other malignancies is being explored. We determined the crystal structure of the yeast 20S proteasome in complex with bortezomib to establish the specificity and binding mode of bortezomib to the proteasome's different catalytically active sites. This structure should enable the rational design of new boronic acid derivatives with improved affinities and specificities for individual active subunits.
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==About this Structure==
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Crystal structure of the boronic acid-based proteasome inhibitor bortezomib in complex with the yeast 20S proteasome.,Groll M, Berkers CR, Ploegh HL, Ovaa H Structure. 2006 Mar;14(3):451-6. PMID:16531229<ref>PMID:16531229</ref>
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2F16 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Saccharomyces_cerevisiae Saccharomyces cerevisiae] with BO2 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Proteasome_endopeptidase_complex Proteasome endopeptidase complex], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.25.1 3.4.25.1] Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2F16 OCA].
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==Reference==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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Crystal structure of the boronic acid-based proteasome inhibitor bortezomib in complex with the yeast 20S proteasome., Groll M, Berkers CR, Ploegh HL, Ovaa H, Structure. 2006 Mar;14(3):451-6. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16531229 16531229]
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</div>
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[[Category: Proteasome endopeptidase complex]]
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<div class="pdbe-citations 2f16" style="background-color:#fffaf0;"></div>
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[[Category: Protein complex]]
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[[Category: Saccharomyces cerevisiae]]
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[[Category: Groll, M.]]
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[[Category: BO2]]
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[[Category: beta-sandwich flanked by helices]]
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[[Category: complex structure covalently bound to the synthetic inihibtor bortezomib]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Wed Nov 21 10:17:26 2007''
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==See Also==
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*[[Proteasome 3D structures|Proteasome 3D structures]]
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Large Structures]]
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[[Category: Saccharomyces cerevisiae]]
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[[Category: Groll M]]

Current revision

Crystal structure of the yeast 20S proteasome in complex with bortezomib

PDB ID 2f16

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