7ps9
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Cereblon isoform 4 from Magnetospirillum gryphiswaldense in complex with Iberdomide (CC-220)== | |
| + | <StructureSection load='7ps9' size='340' side='right'caption='[[7ps9]], [[Resolution|resolution]] 1.80Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[7ps9]] 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=7PS9 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7PS9 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]] 1.8Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=8W7:(3S)-3-[4-({4-[(MORPHOLIN-4-YL)METHYL]PHENYL}METHOXY)-1-OXO-1,3-DIHYDRO-2H-ISOINDOL-2-YL]PIPERIDINE-2,6-DIONE'>8W7</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=7ps9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7ps9 OCA], [https://pdbe.org/7ps9 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7ps9 RCSB], [https://www.ebi.ac.uk/pdbsum/7ps9 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7ps9 ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/A4TVL0_9PROT A4TVL0_9PROT] | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Cereblon (CRBN) is the substrate receptor of the CRL4(CRBN) E3 ubiquitin ligase and is a central player in targeted protein degradation. It is the target of the thalidomide-derived immunomodulatory drugs (IMiDs) and is one of the most widely employed receptors for proteolysis-targeting chimeras (PROTACs), both of which induce the ubiquitination and subsequent proteasomal degradation of target proteins. Structural studies of ligand binding to CRBN are crucial to elucidate the mechanisms of action and for mediation of side effects, ultimately aiding the development of next-generation IMiDs and PROTACs. With this aim, a crystal-soaking system based on the single-domain bacterial homologue MsCI4 has previously been established and used to delineate the binding modes of several classes of small molecules, including FDA-approved drugs, at the molecular level. Here, this system was used to characterize the binding of the next-generation IMiDs avadomide (CC-122) and iberdomide (CC-220) at high resolution, highlighting the advantages and limitations of the MsCI4 system and its implications for the development of future cereblon effectors. | ||
| - | + | High-resolution structures of the bound effectors avadomide (CC-122) and iberdomide (CC-220) highlight advantages and limitations of the MsCI4 soaking system.,Heim C, Hartmann MD Acta Crystallogr D Struct Biol. 2022 Mar 1;78(Pt 3):290-298. doi:, 10.1107/S2059798322000092. Epub 2022 Feb 18. PMID:35234143<ref>PMID:35234143</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| + | <div class="pdbe-citations 7ps9" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Magnetospirillum gryphiswaldense]] | ||
| + | [[Category: Hartmann MD]] | ||
| + | [[Category: Heim C]] | ||
Current revision
Cereblon isoform 4 from Magnetospirillum gryphiswaldense in complex with Iberdomide (CC-220)
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