3shj: Difference between revisions
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[[ | ==Proteasome in complex with hydroxyurea derivative HU10== | ||
<StructureSection load='3shj' size='340' side='right' caption='[[3shj]], [[Resolution|resolution]] 2.80Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[3shj]] 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=3SHJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3SHJ FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=H10:1-HYDROXY-1-[(2R)-4-{3-[(3S,5S,7S)-TRICYCLO[3.3.1.1~3,7~]DEC-1-YLOXY]PHENYL}BUT-3-YN-2-YL]UREA'>H10</scene>, <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</scene></td></tr> | |||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1ryp|1ryp]]</td></tr> | |||
<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> | |||
<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=3shj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3shj OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3shj RCSB], [http://www.ebi.ac.uk/pdbsum/3shj PDBsum]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Inhibitors with a new mechanism of action are needed for 20S proteasome (CP) inhibition owing to the ineffectiveness of current market drugs against some types of solid tumors. A novel class of nonpeptidic CP inhibitors has been developed, which display reversible and noncovalent binding. The structure-based design of these highly active and site-specific inhibitors revealed unexplored binding subpockets. | |||
Hydroxyureas as Noncovalent Proteasome Inhibitors.,Gallastegui N, Beck P, Arciniega M, Huber R, Hillebrand S, Groll M Angew Chem Int Ed Engl. 2011 Nov 21. doi: 10.1002/anie.201106010. PMID:22105886<ref>PMID:22105886</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
==See Also== | ==See Also== | ||
*[[Proteasome|Proteasome]] | *[[Proteasome|Proteasome]] | ||
== References == | |||
== | <references/> | ||
< | __TOC__ | ||
</StructureSection> | |||
[[Category: Proteasome endopeptidase complex]] | [[Category: Proteasome endopeptidase complex]] | ||
[[Category: Saccharomyces cerevisiae]] | [[Category: Saccharomyces cerevisiae]] | ||
[[Category: Arciniega, M | [[Category: Arciniega, M]] | ||
[[Category: Beck, P | [[Category: Beck, P]] | ||
[[Category: Gallastegui, N | [[Category: Gallastegui, N]] | ||
[[Category: Groll, M | [[Category: Groll, M]] | ||
[[Category: Hillebrand, S | [[Category: Hillebrand, S]] | ||
[[Category: Huber, R | [[Category: Huber, R]] | ||
[[Category: Cancer]] | [[Category: Cancer]] | ||
[[Category: Drug development]] | [[Category: Drug development]] | ||
Revision as of 12:32, 9 December 2014
Proteasome in complex with hydroxyurea derivative HU10
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