9brk

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'''Unreleased structure'''
 
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The entry 9brk is ON HOLD
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==Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 in Complex with GRL098-22==
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<StructureSection load='9brk' size='340' side='right'caption='[[9brk]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
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Authors: Chen, Y., Tesmer, J.J.G.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[9brk]] 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=9BRK OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=9BRK FirstGlance]. <br>
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Description: Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 in Complex with GRL098-22
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.7&#8491;</td></tr>
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[[Category: Unreleased Structures]]
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=A1ARA:tert-butyl+(3R)-3-({5-[(Z)-(5-{[(1R)-1-(4-fluorophenyl)ethyl]carbamoyl}-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrol-3-yl}carbamoyl)piperazine-1-carboxylate'>A1ARA</scene></td></tr>
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[[Category: Chen, Y]]
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=9brk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=9brk OCA], [https://pdbe.org/9brk PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=9brk RCSB], [https://www.ebi.ac.uk/pdbsum/9brk PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=9brk ProSAT]</span></td></tr>
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[[Category: Tesmer, J.J.G]]
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</table>
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== Function ==
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[https://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: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Chen Y]]
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[[Category: Tesmer JJG]]

Current revision

Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 in Complex with GRL098-22

PDB ID 9brk

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