4tnd
From Proteopedia
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| - | ''' | + | ==Crystal Structure of G Protein-Coupled Receptor Kinase 5 in Complex with AMP-PNP== | 
| - | + | <StructureSection load='4tnd' size='340' side='right' caption='[[4tnd]], [[Resolution|resolution]] 1.80Å' scene=''> | |
| - | + | == Structural highlights == | |
| - | + | <table><tr><td colspan='2'>[[4tnd]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4TND OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4TND FirstGlance]. <br> | |
| - | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ANP:PHOSPHOAMINOPHOSPHONIC+ACID-ADENYLATE+ESTER'>ANP</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr> | |
| - | + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4tnb|4tnb]]</td></tr> | |
| - | + | <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> | |
| - | [[Category:  | + | <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=4tnd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4tnd OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4tnd RCSB], [http://www.ebi.ac.uk/pdbsum/4tnd PDBsum]</span></td></tr> | 
| + | </table> | ||
| + | == Function == | ||
| + | [[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>   | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Benovic, J L]] | ||
| [[Category: Bhardwaj, A]] | [[Category: Bhardwaj, A]] | ||
| - | [[Category:  | + | [[Category: Komolov, K E]] | 
| - | [[Category:  | + | [[Category: Gpcr kinase]] | 
| + | [[Category: Gpcr kinase 5]] | ||
| + | [[Category: Kinase]] | ||
Revision as of 14:07, 10 June 2015
Crystal Structure of G Protein-Coupled Receptor Kinase 5 in Complex with AMP-PNP
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