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8gcy
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Co-crystal structure of CBL-B in complex with N-Aryl isoindolin-1-one inhibitor== | |
| - | + | <StructureSection load='8gcy' size='340' side='right'caption='[[8gcy]], [[Resolution|resolution]] 1.81Å' scene=''> | |
| - | + | == Structural highlights == | |
| - | + | <table><tr><td colspan='2'>[[8gcy]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8GCY OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8GCY FirstGlance]. <br> | |
| - | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</scene>, <scene name='pdbligand=Z3N:2-{3-[(1s,3R)-3-methyl-1-(4-methyl-4H-1,2,4-triazol-3-yl)cyclobutyl]phenyl}-6-{[(3S)-3-methylpiperidin-1-yl]methyl}-4-(trifluoromethyl)-2,3-dihydro-1H-isoindol-1-one'>Z3N</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr> | |
| - | [[Category: | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=8gcy FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8gcy OCA], [https://pdbe.org/8gcy PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8gcy RCSB], [https://www.ebi.ac.uk/pdbsum/8gcy PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8gcy ProSAT]</span></td></tr> |
| - | [[Category: | + | </table> |
| - | [[Category: Arrowsmith | + | == Function == |
| - | [[Category: | + | [https://www.uniprot.org/uniprot/CBLB_HUMAN CBLB_HUMAN] E3 ubiquitin-protein ligase which accepts ubiquitin from specific E2 ubiquitin-conjugating enzymes, and transfers it to substrates, generally promoting their degradation by the proteasome. Negatively regulates TCR (T-cell receptor), BCR (B-cell receptor) and FCER1 (high affinity immunoglobulin epsilon receptor) signal transduction pathways. In naive T-cells, inhibits VAV1 activation upon TCR engagement and imposes a requirement for CD28 costimulation for proliferation and IL-2 production. Also acts by promoting PIK3R1/p85 ubiquitination, which impairs its recruitment to the TCR and subsequent activation. In activated T-cells, inhibits PLCG1 activation and calcium mobilization upon restimulation and promotes anergy. In B-cells, acts by ubiquitinating SYK and promoting its proteasomal degradation. May also be involved in EGFR ubiquitination and internalization.<ref>PMID:10022120</ref> <ref>PMID:10086340</ref> <ref>PMID:11087752</ref> <ref>PMID:11526404</ref> |
| - | [[Category: | + | == References == |
| - | [[Category: | + | <references/> |
| - | [[Category: | + | __TOC__ |
| - | [[Category: | + | </StructureSection> |
| - | [[Category: | + | [[Category: Homo sapiens]] |
| - | [[Category: Zeng | + | [[Category: Large Structures]] |
| + | [[Category: Arrowsmith CH]] | ||
| + | [[Category: Dong A]] | ||
| + | [[Category: Edwards AM]] | ||
| + | [[Category: Halabelian L]] | ||
| + | [[Category: Kimani S]] | ||
| + | [[Category: Li Y]] | ||
| + | [[Category: Santhakumar V]] | ||
| + | [[Category: Zeng H]] | ||
Revision as of 07:27, 22 March 2023
Co-crystal structure of CBL-B in complex with N-Aryl isoindolin-1-one inhibitor
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Categories: Homo sapiens | Large Structures | Arrowsmith CH | Dong A | Edwards AM | Halabelian L | Kimani S | Li Y | Santhakumar V | Zeng H
