5oh3: Difference between revisions
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==Cereblon isoform 4 from Magnetospirillum gryphiswaldense in complex with Ethosuximide== | ==Cereblon isoform 4 from Magnetospirillum gryphiswaldense in complex with Ethosuximide== | ||
<StructureSection load='5oh3' size='340' side='right' caption='[[5oh3]], [[Resolution|resolution]] 2.10Å' scene=''> | <StructureSection load='5oh3' size='340' side='right'caption='[[5oh3]], [[Resolution|resolution]] 2.10Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[5oh3]] is a 3 chain structure with sequence from [ | <table><tr><td colspan='2'>[[5oh3]] 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=5OH3 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5OH3 FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=9V2:(3~{S})-3-ethyl-3-methyl-pyrrolidine-2,5-dione'>9V2</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene> | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.1Å</td></tr> | ||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=9V2:(3~{S})-3-ethyl-3-methyl-pyrrolidine-2,5-dione'>9V2</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'>[ | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5oh3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5oh3 OCA], [https://pdbe.org/5oh3 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5oh3 RCSB], [https://www.ebi.ac.uk/pdbsum/5oh3 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5oh3 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 5oh3" style="background-color:#fffaf0;"></div> | |||
== References == | |||
<references/> | |||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: | [[Category: Large Structures]] | ||
[[Category: | [[Category: Magnetospirillum gryphiswaldense]] | ||
[[Category: | [[Category: Albrecht R]] | ||
[[Category: Boichenko | [[Category: Boichenko I]] | ||
[[Category: Hartmann | [[Category: Hartmann MD]] | ||
[[Category: | [[Category: Hernandez Alvarez B]] | ||
[[Category: | [[Category: Lupas AN]] | ||
Latest revision as of 16:50, 13 December 2023
Cereblon isoform 4 from Magnetospirillum gryphiswaldense in complex with Ethosuximide
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