3un8

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[[Image:3un8.png|left|200px]]
 
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==Yeast 20S proteasome in complex with PR-957 (epoxide)==
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The line below this paragraph, containing "STRUCTURE_3un8", creates the "Structure Box" on the page.
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<StructureSection load='3un8' size='340' side='right'caption='[[3un8]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3un8]] is a 20 chain structure with sequence from [https://en.wikipedia.org/wiki/Saccharomyces_cerevisiae_S288C Saccharomyces cerevisiae S288C]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3UN8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3UN8 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]] 2.7&#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=049:2-(ACETYLAMINO)-4,5-ANHYDRO-1,2-DIDEOXY-4-METHYL-1-PHENYL-D-XYLITOL'>049</scene></td></tr>
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{{STRUCTURE_3un8| PDB=3un8 | 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=3un8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3un8 OCA], [https://pdbe.org/3un8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3un8 RCSB], [https://www.ebi.ac.uk/pdbsum/3un8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3un8 ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/PSA4_YEAST PSA4_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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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Constitutive proteasomes and immunoproteasomes shape the peptide repertoire presented by major histocompatibility complex class I (MHC-I) molecules by harboring different sets of catalytically active subunits. Here, we present the crystal structures of constitutive proteasomes and immunoproteasomes from mouse in the presence and absence of the epoxyketone inhibitor PR-957 (ONX 0914) at 2.9 A resolution. Based on our X-ray data, we propose a unique catalytic feature for the immunoproteasome subunit beta5i/LMP7. Comparison of ligand-free and ligand-bound proteasomes reveals conformational changes in the S1 pocket of beta5c/X but not beta5i, thereby explaining the selectivity of PR-957 for beta5i. Time-resolved structures of yeast proteasome:PR-957 complexes indicate that ligand docking to the active site occurs only via the reactive head group and the P1 side chain. Together, our results support structure-guided design of inhibitory lead structures selective for immunoproteasomes that are linked to cytokine production and diseases like cancer and autoimmune disorders.
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===Yeast 20S proteasome in complex with PR-957 (epoxide)===
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Immuno- and constitutive proteasome crystal structures reveal differences in substrate and inhibitor specificity.,Huber EM, Basler M, Schwab R, Heinemeyer W, Kirk CJ, Groettrup M, Groll M Cell. 2012 Feb 17;148(4):727-38. PMID:22341445<ref>PMID:22341445</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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<div class="pdbe-citations 3un8" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Proteasome 3D structures|Proteasome 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 22341445 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_22341445}}
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__TOC__
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</StructureSection>
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==About this Structure==
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[[Category: Large Structures]]
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[[3un8]] is a 28 chain structure with sequence from [http://en.wikipedia.org/wiki/Saccharomyces_cerevisiae Saccharomyces cerevisiae]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3UN8 OCA].
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[[Category: Saccharomyces cerevisiae S288C]]
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[[Category: Basler M]]
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==Reference==
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[[Category: Groettrup M]]
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<ref group="xtra">PMID:022341445</ref><references group="xtra"/>
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[[Category: Groll M]]
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[[Category: Proteasome endopeptidase complex]]
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[[Category: Heinemeyer W]]
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[[Category: Saccharomyces cerevisiae]]
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[[Category: Huber E]]
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[[Category: Basler, M.]]
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[[Category: Kirk C]]
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[[Category: Groettrup, M.]]
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[[Category: Schwab R]]
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[[Category: Groll, M.]]
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[[Category: Heinemeyer, W.]]
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[[Category: Huber, E.]]
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[[Category: Kirk, C.]]
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[[Category: Schwab, R.]]
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[[Category: Antigen presentation]]
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[[Category: Drug development]]
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[[Category: Hydrolase-hydrolase inhibtior complex]]
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[[Category: Proteasome]]
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[[Category: Protein degradation]]
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Current revision

Yeast 20S proteasome in complex with PR-957 (epoxide)

PDB ID 3un8

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