5w5j

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m (Protected "5w5j" [edit=sysop:move=sysop])
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'''Unreleased structure'''
 
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The entry 5w5j is ON HOLD until Paper Publication
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==Identification of potent and selective RIPK2 inhibitors for the treatment of inflammatory diseases==
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<StructureSection load='5w5j' size='340' side='right' caption='[[5w5j]], [[Resolution|resolution]] 2.85&Aring;' scene=''>
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Authors:
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5w5j]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5W5J OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5W5J FirstGlance]. <br>
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Description:
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=9WS:N-(2-chlorophenyl)pyrazolo[1,5-a]pyridine-3-carboxamide'>9WS</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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[[Category: Unreleased Structures]]
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5w5w|5w5w]]</td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] </span></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=5w5j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5w5j OCA], [http://pdbe.org/5w5j PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5w5j RCSB], [http://www.ebi.ac.uk/pdbsum/5w5j PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5w5j ProSAT]</span></td></tr>
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</table>
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== Function ==
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[[http://www.uniprot.org/uniprot/RIPK2_HUMAN RIPK2_HUMAN]] Serine/threonine/tyrosine kinase that plays an essential role in modulation of innate and adaptive immune responses. Upon stimulation by bacterial peptidoglycans, NOD1 and NOD2 are activated, oligomerize and recruit RIPK2 through CARD-CARD domains. Once recruited, RIPK2 autophosphorylates and undergoes 'Lys-63'-linked polyubiquitination by E3 ubiquitin ligases BIRC2 and BIRC3. The polyubiquitinated protein mediates the recruitment of MAP3K7/TAK1 to IKBKG/NEMO and induces 'Lys-63'-linked polyubiquitination of IKBKG/NEMO and subsequent activation of IKBKB/IKKB. In turn, NF-kappa-B is released from NF-kappa-B inhibitors and translocates into the nucleus where it activates the transcription of hundreds of genes involved in immune response, growth control, or protection against apoptosis. Plays also a role during engagement of the T-cell receptor (TCR) in promoting BCL10 phosphorylation and subsequent NF-kappa-B activation.<ref>PMID:14638696</ref> <ref>PMID:17054981</ref> <ref>PMID:18079694</ref> <ref>PMID:21123652</ref>
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Non-specific protein-tyrosine kinase]]
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[[Category: Kreusch, A]]
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[[Category: Spraggon, G]]
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[[Category: Complex]]
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[[Category: Hydrolase]]
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[[Category: Hydrolase-hydrolase inhibitor complex]]
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[[Category: Inhibitor]]
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[[Category: Kinase]]

Revision as of 07:17, 25 October 2017

Identification of potent and selective RIPK2 inhibitors for the treatment of inflammatory diseases

5w5j, resolution 2.85Å

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