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==Crystal structure of yeast CP in complex with Belactosin C== | |||
<StructureSection load='3tdd' size='340' side='right'caption='[[3tdd]], [[Resolution|resolution]] 2.70Å' scene=''> | |||
== Structural highlights == | |||
<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> | |||
</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=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> | |||
<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> | |||
</table> | |||
== Function == | |||
[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. | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
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. | |||
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> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
<div class="pdbe-citations 3tdd" style="background-color:#fffaf0;"></div> | |||
==See Also== | ==See Also== | ||
*[[Proteasome|Proteasome]] | *[[Proteasome 3D structures|Proteasome 3D structures]] | ||
== References == | |||
== | <references/> | ||
< | __TOC__ | ||
[[Category: | </StructureSection> | ||
[[Category: Saccharomyces cerevisiae]] | [[Category: Large Structures]] | ||
[[Category: Groll | [[Category: Saccharomyces cerevisiae S288C]] | ||
[[Category: Korotkov | [[Category: Groll M]] | ||
[[Category: Larionov | [[Category: Korotkov VS]] | ||
[[Category: Ludwig | [[Category: Larionov OV]] | ||
[[Category: Lygin | [[Category: Ludwig A]] | ||
[[Category: Meijere | [[Category: Lygin AV]] | ||
[[Category: De Meijere A]] | |||
Latest revision as of 05:27, 21 November 2024
Crystal structure of yeast CP in complex with Belactosin CCrystal structure of yeast CP in complex with Belactosin C
Structural highlights
FunctionPSA4_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. Publication Abstract from PubMedSuccessful 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. 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[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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