4r18

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'''Unreleased structure'''
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==Ligand-induced Lys33-Thr1 crosslinking at subunit beta5 of the yeast 20S proteasome==
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<StructureSection load='4r18' size='340' side='right' caption='[[4r18]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4r18]] is a 28 chain structure with sequence from [http://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=4R18 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4R18 FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ABA:ALPHA-AMINOBUTYRIC+ACID'>ABA</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1ryp|1ryp]], [[4r17|4r17]]</td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[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] </span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4r18 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4r18 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4r18 RCSB], [http://www.ebi.ac.uk/pdbsum/4r18 PDBsum]</span></td></tr>
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</table>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The concept of proteasome inhibition ranks among the latest achievements in the treatment of blood cancer and represents a promising strategy for modulating autoimmune diseases. In this study, we describe peptidic sulfonyl fluoride inhibitors that selectively block the catalytic beta5 subunit of the immunoproteasome by inducing only marginal cytotoxic effects. Structural and mass spectrometric analyses revealed a novel reaction mechanism involving polarity inversion and irreversible crosslinking of the proteasomal active site. We thus identified the sulfonyl fluoride headgroup for the development and optimization of immunoproteasome selective compounds and their possible application in autoimmune disorders.
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The entry 4r18 is ON HOLD
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Selective Inhibition of the Immunoproteasome by Ligand-Induced Crosslinking of the Active Site.,Dubiella C, Cui H, Gersch M, Brouwer AJ, Sieber SA, Kruger A, Liskamp RM, Groll M Angew Chem Int Ed Engl. 2014 Sep 22. doi: 10.1002/anie.201406964. PMID:25244435<ref>PMID:25244435</ref>
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Authors: Dubiella, C., Cui, H., Gersch, M., Brouwer, A.J., Sieber, S.A., Krueger, A., Liskamp, R., Groll, M.
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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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Description: Ligand-induced Lys33-Thr1 crosslinking at subunit beta5 of the yeast 20S proteasome
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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: Proteasome endopeptidase complex]]
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[[Category: Saccharomyces cerevisiae s288c]]
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[[Category: Brouwer, A J.]]
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[[Category: Cui, H.]]
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[[Category: Dubiella, C.]]
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[[Category: Gersch, M.]]
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[[Category: Groll, M.]]
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[[Category: Krueger, A.]]
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[[Category: Liskamp, R.]]
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[[Category: Sieber, S A.]]
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[[Category: Binding analysis]]
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[[Category: Crosslink]]
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[[Category: Drug development]]
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[[Category: Hydrolase-hydrolase inhibitor complex]]
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[[Category: Proteasome]]
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[[Category: Umpolung]]

Revision as of 10:44, 20 October 2014

Ligand-induced Lys33-Thr1 crosslinking at subunit beta5 of the yeast 20S proteasome

4r18, resolution 2.40Å

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