4q1s
From Proteopedia
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| - | ''' | + | ==Yeast 20S proteasome in Complex with Kendomycin== |
| + | <StructureSection load='4q1s' size='340' side='right' caption='[[4q1s]], [[Resolution|resolution]] 2.60Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[4q1s]] 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=4Q1S OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4Q1S FirstGlance]. <br> | ||
| + | </td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2YD:(5R,6R,7S,8R,9R,12S,13E,16S,18S,19R,20AR)-4,7,19-TRIHYDROXY-2,6,8,12,14,16,18-HEPTAMETHYL-6,7,8,9,10,11,12,15,16,17,18,19,20,20A-TETRADECAHYDRO-1,19 5,9-DIEPOXYBENZO[18]ANNULEN-3(5H)-ONE'>2YD</scene><br> | ||
| + | <tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1ryp|1ryp]]</td></tr> | ||
| + | <tr><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><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4q1s FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4q1s OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4q1s RCSB], [http://www.ebi.ac.uk/pdbsum/4q1s PDBsum]</span></td></tr> | ||
| + | <table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Natural products are a valuable source for novel lead structures in drug discovery, but for the majority of isolated bioactive compounds the cellular targets are unknown. The structurally unique ansa-polyketide kendomycin was reported to exert its potent cytotoxic effects via impairment of the ubiquitin proteasome system, but the exact mode of action remained unclear. Here, we present a systematic biochemical characterization of kendomycin-proteasome interactions in vitro as well as in vivo, including complex structures of wildtype and mutant yeast 20S proteasome with kendomycin. Our results provide evidence for a polypharmacological mode of action for kendomycin's cytotoxic effect on cancer cells. | ||
| - | + | Structural and biochemical characterization of the natural product kendomycin and the 20S proteasome.,Beck P, Heinemeyer W, Spath AL, Elnakady Y, Muller R, Groll M J Mol Biol. 2014 Jul 16. pii: S0022-2836(14)00335-0. doi:, 10.1016/j.jmb.2014.06.019. PMID:25038530<ref>PMID:25038530</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | == References == | |
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Proteasome endopeptidase complex]] | ||
| + | [[Category: Saccharomyces cerevisiae]] | ||
| + | [[Category: Beck, P.]] | ||
| + | [[Category: Elnakady, Y.]] | ||
| + | [[Category: Groll, M.]] | ||
| + | [[Category: Heinemeyer, W.]] | ||
| + | [[Category: Mueller, R.]] | ||
| + | [[Category: Spaeth, A.]] | ||
| + | [[Category: Covalent binding]] | ||
| + | [[Category: Exosite]] | ||
| + | [[Category: Hydrolase-toxin complex]] | ||
| + | [[Category: Natural product]] | ||
| + | [[Category: Proteasome]] | ||
| + | [[Category: Quinone methide]] | ||
Revision as of 07:36, 30 July 2014
Yeast 20S proteasome in Complex with Kendomycin
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