4i1r

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{{STRUCTURE_4i1r| PDB=4i1r | SCENE= }}
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==Human MALT1 (caspase-IG3) in complex with thioridazine==
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===Human MALT1 (caspase-IG3) in complex with thioridazine===
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<StructureSection load='4i1r' size='340' side='right' caption='[[4i1r]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
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{{ABSTRACT_PUBMED_23946259}}
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4i1r]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4I1R OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4I1R FirstGlance]. <br>
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==Disease==
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=LZU:10-{2-[(2S)-1-METHYLPIPERIDIN-2-YL]ETHYL}-2-(METHYLSULFANYL)-10H-PHENOTHIAZINE'>LZU</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4i1p|4i1p]]</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">MALT1, MLT ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4i1r FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4i1r OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4i1r RCSB], [http://www.ebi.ac.uk/pdbsum/4i1r PDBsum]</span></td></tr>
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</table>
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== Disease ==
[[http://www.uniprot.org/uniprot/MALT1_HUMAN MALT1_HUMAN]] Note=A chromosomal aberration involving MALT1 is recurrent in low-grade mucosa-associated lymphoid tissue (MALT lymphoma). Translocation t(11;18)(q21;q21) with BIRC2. This translocation is found in approximately 50% of cytogenetically abnormal low-grade MALT lymphoma.
[[http://www.uniprot.org/uniprot/MALT1_HUMAN MALT1_HUMAN]] Note=A chromosomal aberration involving MALT1 is recurrent in low-grade mucosa-associated lymphoid tissue (MALT lymphoma). Translocation t(11;18)(q21;q21) with BIRC2. This translocation is found in approximately 50% of cytogenetically abnormal low-grade MALT lymphoma.
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== Function ==
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==Function==
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[[http://www.uniprot.org/uniprot/MALT1_HUMAN MALT1_HUMAN]] Enhances BCL10-induced activation of NF-kappa-B. Involved in nuclear export of BCL10. Binds to TRAF6, inducing TRAF6 oligomerization and activation of its ligase activity. Has ubiquitin ligase activity. MALT1-dependent BCL10 cleavage plays an important role in T-cell antigen receptor-induced integrin adhesion.<ref>PMID:11262391</ref> <ref>PMID:14695475</ref> <ref>PMID:18264101</ref>
[[http://www.uniprot.org/uniprot/MALT1_HUMAN MALT1_HUMAN]] Enhances BCL10-induced activation of NF-kappa-B. Involved in nuclear export of BCL10. Binds to TRAF6, inducing TRAF6 oligomerization and activation of its ligase activity. Has ubiquitin ligase activity. MALT1-dependent BCL10 cleavage plays an important role in T-cell antigen receptor-induced integrin adhesion.<ref>PMID:11262391</ref> <ref>PMID:14695475</ref> <ref>PMID:18264101</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Second site: In the crystal structure of human MALT1casp-Ig3 (mucosa-associated lymphoid tissue lymphoma translocation protein 1) in complex with the tricyclic phenothiazine derivative thioridazine (violet in the picture), the inhibitor is bound in a hydrophobic pocket far from the active site. This explains the action of phenothiazine derivatives as noncompetitive, reversible inhibitors.
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==About this Structure==
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Structural Analysis of Phenothiazine Derivatives as Allosteric Inhibitors of the MALT1 Paracaspase.,Schlauderer F, Lammens K, Nagel D, Vincendeau M, Eitelhuber AC, Verhelst SH, Kling D, Chrusciel A, Ruland J, Krappmann D, Hopfner KP Angew Chem Int Ed Engl. 2013 Aug 14. doi: 10.1002/anie.201304290. PMID:23946259<ref>PMID:23946259</ref>
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[[4i1r]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4I1R OCA].
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==Reference==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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<ref group="xtra">PMID:023946259</ref><references group="xtra"/><references/>
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</div>
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== References ==
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<references/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Hopfner, K P.]]
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[[Category: Hopfner, K P]]
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[[Category: Lammens, K.]]
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[[Category: Lammens, K]]
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[[Category: Schlauderer, F.]]
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[[Category: Schlauderer, F]]
[[Category: Hydrolase-hydrolase inhibitor complex]]
[[Category: Hydrolase-hydrolase inhibitor complex]]
[[Category: Protease]]
[[Category: Protease]]

Revision as of 13:05, 5 January 2015

Human MALT1 (caspase-IG3) in complex with thioridazine

4i1r, resolution 2.70Å

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