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3tdd

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==Crystal structure of yeast CP in complex with Belactosin C==
==Crystal structure of yeast CP in complex with Belactosin C==
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<StructureSection load='3tdd' size='340' side='right' caption='[[3tdd]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
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<StructureSection load='3tdd' size='340' side='right'caption='[[3tdd]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[3tdd]] 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=3TDD OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3TDD FirstGlance]. <br>
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<table><tr><td colspan='2'>[[3tdd]] 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=3TDD OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3TDD 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=BFO:BENZYL+N-[(NAPHTHALEN-2-YLMETHOXY)CARBONYL]-L-ALANYL-N~5~-[(2R,3S,4S)-3-FORMYL-2-HYDROXY-4-METHYLHEXANOYL]-L-ORNITHINATE'>BFO</scene></td></tr>
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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='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1ryp|1ryp]], [[3e47|3e47]]</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=BFO:BENZYL+N-[(NAPHTHALEN-2-YLMETHOXY)CARBONYL]-L-ALANYL-N~5~-[(2R,3S,4S)-3-FORMYL-2-HYDROXY-4-METHYLHEXANOYL]-L-ORNITHINATE'>BFO</scene></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'>[https://proteopedia.org/fgij/fg.htm?mol=3tdd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3tdd OCA], [https://pdbe.org/3tdd PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3tdd RCSB], [https://www.ebi.ac.uk/pdbsum/3tdd PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3tdd ProSAT]</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=3tdd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3tdd OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3tdd RCSB], [http://www.ebi.ac.uk/pdbsum/3tdd PDBsum]</span></td></tr>
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</table>
</table>
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<div style="background-color:#fffaf0;">
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== Function ==
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== Publication Abstract from PubMed ==
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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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Successful biochemical studies of the natural products belactosin A and C as well as their more stable acylated derivatives have proved them to be powerful proteasome inhibitors and thereby potential candidates as pharmacologically relevant active compounds. In order to understand their structure-biological activity relations in detail and to find ways of improving their biological activity, four new modified belactosin congeners have been synthesized and tested. One of them (compound 6) turned out to be a more potent inhibitor against HeLa cells than the known proteasome inhibitor MG132.
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Synthesis and biological activity of optimized belactosin C congeners.,Korotkov VS, Ludwig A, Larionov OV, Lygin AV, Groll M, de Meijere A Org Biomol Chem. 2011 Sep 23. PMID:21946808<ref>PMID:21946808</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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==See Also==
==See Also==
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*[[Proteasome|Proteasome]]
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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__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Proteasome endopeptidase complex]]
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[[Category: Large Structures]]
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[[Category: Saccharomyces cerevisiae]]
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[[Category: Saccharomyces cerevisiae S288C]]
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[[Category: Groll, M]]
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[[Category: Groll M]]
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[[Category: Korotkov, V S]]
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[[Category: Korotkov VS]]
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[[Category: Larionov, O V]]
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[[Category: Larionov OV]]
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[[Category: Ludwig, A]]
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[[Category: Ludwig A]]
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[[Category: Lygin, A V]]
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[[Category: Lygin AV]]
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[[Category: Meijere, A de]]
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[[Category: De Meijere A]]
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[[Category: Beta-sandwich flanked by alpha-helice]]
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[[Category: Drug development]]
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[[Category: Hydrolase]]
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[[Category: Hydrolase-hydrolase inhibitor complex]]
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[[Category: Inhibitor]]
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[[Category: Primed substrate binding channel]]
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[[Category: Proteasome]]
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[[Category: Ubiquitin]]
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Current revision

Crystal structure of yeast CP in complex with Belactosin C

PDB ID 3tdd

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