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5oha
From Proteopedia
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==Cereblon isoform 4 from Magnetospirillum gryphiswaldense in complex with 2-Thiohydantoin== | ==Cereblon isoform 4 from Magnetospirillum gryphiswaldense in complex with 2-Thiohydantoin== | ||
| - | <StructureSection load='5oha' size='340' side='right' caption='[[5oha]], [[Resolution|resolution]] 1.55Å' scene=''> | + | <StructureSection load='5oha' size='340' side='right'caption='[[5oha]], [[Resolution|resolution]] 1.55Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[5oha]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5OHA OCA]. For a <b>guided tour on the structure components</b> use [ | + | <table><tr><td colspan='2'>[[5oha]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/Magnetospirillum_gryphiswaldense Magnetospirillum gryphiswaldense]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5OHA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5OHA FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=9UW:2-sulfanylideneimidazol-4-one'>9UW</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.55Å</td></tr> |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=9UW:2-sulfanylideneimidazol-4-one'>9UW</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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=5oha FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5oha OCA], [https://pdbe.org/5oha PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5oha RCSB], [https://www.ebi.ac.uk/pdbsum/5oha PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5oha ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/A4TVL0_9PROT A4TVL0_9PROT] | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | The protein cereblon serves as a substrate receptor of a ubiquitin ligase complex that can be tuned toward different target proteins by cereblon-binding agents. This approach to targeted protein degradation is exploited in different clinical settings and has sparked the development of a growing number of thalidomide derivatives. Here, we probe the chemical space of cereblon binding beyond such derivatives and work out a simple set of chemical requirements, delineating the metaclass of cereblon effectors. We report co-crystal structures for a diverse set of compounds, including commonly used pharmaceuticals, but also find that already minimalistic cereblon-binding moieties might exert teratogenic effects in zebrafish. Our results may guide the design of a post-thalidomide generation of therapeutic cereblon effectors and provide a framework for the circumvention of unintended cereblon binding by negative design for future pharmaceuticals. | ||
| + | |||
| + | Chemical Ligand Space of Cereblon.,Boichenko I, Bar K, Deiss S, Heim C, Albrecht R, Lupas AN, Hernandez Alvarez B, Hartmann MD ACS Omega. 2018 Sep 14;3(9):11163-11171. doi: 10.1021/acsomega.8b00959. , eCollection 2018 Sep 30. PMID:31459225<ref>PMID:31459225</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 5oha" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: | + | [[Category: Large Structures]] |
| - | [[Category: | + | [[Category: Magnetospirillum gryphiswaldense]] |
| - | [[Category: | + | [[Category: Albrecht R]] |
| - | [[Category: | + | [[Category: Boichenko I]] |
| - | [[Category: | + | [[Category: Hartmann MD]] |
| - | [[Category: | + | [[Category: Hernandez Alvarez B]] |
| - | [[Category: | + | [[Category: Lupas AN]] |
| - | + | ||
| - | + | ||
| - | + | ||
Current revision
Cereblon isoform 4 from Magnetospirillum gryphiswaldense in complex with 2-Thiohydantoin
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