8gcy: Difference between revisions
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==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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