5m2b
From Proteopedia
(Difference between revisions)
(New page: '''Unreleased structure''' The entry 5m2b is ON HOLD Authors: Groll, M. Description: Yeast 20S proteasome with human beta5i (1-138) and human beta6 (97-111; 118-133) in complex with th...) |
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| - | '''Unreleased structure''' | ||
| - | + | ==Yeast 20S proteasome with human beta5i (1-138) and human beta6 (97-111; 118-133) in complex with thiazole based inhibitor Ro19== | |
| + | <StructureSection load='5m2b' size='340' side='right'caption='[[5m2b]], [[Resolution|resolution]] 2.70Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5m2b]] 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=5M2B OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5M2B FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.7Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=7DX:(2~{S})-2-CYCLOHEXYL-4-OXIDANYLIDENE-4-[[7-(4-PHENYL-1,3-THIAZOL-2-YL)QUINOLIN-2-YL]AMINO]BUTANOIC+ACID'>7DX</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5m2b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5m2b OCA], [https://pdbe.org/5m2b PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5m2b RCSB], [https://www.ebi.ac.uk/pdbsum/5m2b PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5m2b ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [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. | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Selective inhibition of the immunoproteasome is a promising approach towards the development of immunomodulatory drugs. Recently, a class of substituted thiazole compounds that combine a non-peptidic scaffold with the absence of an electrophile has been reported in a patent. Herein, we describe the mode of action of the lead compound using a sophisticated chimeric yeast model of the human immunoproteasome for structural studies. The inhibitor adopts a unique orientation perpendicular to the beta5i substrate binding channel. Distinctive interactions between the inhibitor and the subpockets of the human immunoproteasome account for its isotype selectivity. | ||
| - | + | Structural elucidation of a non-peptidic inhibitor specific for the human immunoproteasome.,Cui H, Baur R, Le Chapelain C, Dubiella C, Heinemeyer W, Huber EM, Groll M Chembiochem. 2017 Jan 18. doi: 10.1002/cbic.201700021. PMID:28098422<ref>PMID:28098422</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| - | [[Category: Groll | + | <div class="pdbe-citations 5m2b" style="background-color:#fffaf0;"></div> |
| + | |||
| + | ==See Also== | ||
| + | *[[Proteasome 3D structures|Proteasome 3D structures]] | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Saccharomyces cerevisiae S288C]] | ||
| + | [[Category: Groll M]] | ||
Current revision
Yeast 20S proteasome with human beta5i (1-138) and human beta6 (97-111; 118-133) in complex with thiazole based inhibitor Ro19
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