4tnb

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'''Unreleased structure'''
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==Crystal Structure of G Protein-Coupled Receptor Kinase 5 in Complex with Sangivamycin==
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<StructureSection load='4tnb' size='340' side='right' caption='[[4tnb]], [[Resolution|resolution]] 2.11&Aring;' scene=''>
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The entry 4tnb is ON HOLD until Paper Publication
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4tnb]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4TNB OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4TNB FirstGlance]. <br>
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Authors: Bhardwaj, A., Komolov, K.E., Benovic, J.L.
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SGV:SANGIVAMYCIN'>SGV</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4tnd|4tnd]]</td></tr>
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Description:
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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/[G-protein-coupled_receptor]_kinase [G-protein-coupled receptor] kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.16 2.7.11.16] </span></td></tr>
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[[Category: Unreleased Structures]]
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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=4tnb FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4tnb OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4tnb RCSB], [http://www.ebi.ac.uk/pdbsum/4tnb PDBsum]</span></td></tr>
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</table>
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== Function ==
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[[http://www.uniprot.org/uniprot/GRK5_HUMAN GRK5_HUMAN]] Serine/threonine kinase that phosphorylates preferentially the activated forms of a variety of G-protein-coupled receptors (GPCRs). Such receptor phosphorylation initiates beta-arrestin-mediated receptor desensitization, internalization, and signaling events leading to their down-regulation. Phosphorylates a variety of GPCRs, including adrenergic receptors, muscarinic acetylcholine receptors (more specifically Gi-coupled M2/M4 subtypes), dopamine receptors and opioid receptors. In addition to GPCRs, also phosphorylates various substrates: Hsc70-interacting protein/ST13, TP53/p53, HDAC5, and arrestin-1/ARRB1. Phosphorylation of ARRB1 by GRK5 inhibits G-protein independent MAPK1/MAPK3 signaling downstream of 5HT4-receptors. Phosphorylation of HDAC5, a repressor of myocyte enhancer factor 2 (MEF2) leading to nuclear export of HDAC5 and allowing MEF2-mediated transcription. Phosphorylation of TP53/p53, a crucial tumor suppressor, inhibits TP53/p53-mediated apoptosis. Phosphorylation of ST13 regulates internalization of the chemokine receptor. Phosphorylates rhodopsin (RHO) (in vitro) and a non G-protein-coupled receptor, LRP6 during Wnt signaling (in vitro).<ref>PMID:19661922</ref> <ref>PMID:19801552</ref> <ref>PMID:20038610</ref> <ref>PMID:20124405</ref> <ref>PMID:21728385</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: Benovic, J L]]
[[Category: Bhardwaj, A]]
[[Category: Bhardwaj, A]]
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[[Category: Benovic, J.L]]
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[[Category: Komolov, K E]]
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[[Category: Komolov, K.E]]
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[[Category: Gpcr kinase]]
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[[Category: Grk5-sangivamycin complex]]
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[[Category: Inhibitor]]
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[[Category: Kinase]]

Revision as of 14:07, 10 June 2015

Crystal Structure of G Protein-Coupled Receptor Kinase 5 in Complex with Sangivamycin

4tnb, resolution 2.11Å

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