3krw

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{{Seed}}
 
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[[Image:3krw.jpg|left|200px]]
 
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==Human GRK2 in complex with Gbetgamma subunits and balanol (soak)==
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The line below this paragraph, containing "STRUCTURE_3krw", creates the "Structure Box" on the page.
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<StructureSection load='3krw' size='340' side='right'caption='[[3krw]], [[Resolution|resolution]] 2.90&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[3krw]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/Bos_taurus Bos taurus] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3KRW OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3KRW FirstGlance]. <br>
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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]] 2.9&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=BA1:BALANOL'>BA1</scene>, <scene name='pdbligand=CMT:O-METHYLCYSTEINE'>CMT</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
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{{STRUCTURE_3krw| PDB=3krw | SCENE= }}
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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=3krw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3krw OCA], [https://pdbe.org/3krw PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3krw RCSB], [https://www.ebi.ac.uk/pdbsum/3krw PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3krw ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/ARBK1_HUMAN ARBK1_HUMAN] Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. Key regulator of LPAR1 signaling. Competes with RALA for binding to LPAR1 thus affecting the signaling properties of the receptor. Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner.<ref>PMID:19306925</ref>
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/kr/3krw_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=3krw ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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G protein-coupled receptor kinase 2 (GRK2) is a pharmaceutical target for the treatment of cardiovascular diseases such as congestive heart failure, myocardial infarction, and hypertension. To better understand how nanomolar inhibition and selectivity for GRK2 might be achieved, we have determined crystal structures of human GRK2 in complex with Gbetagamma in the presence and absence of the AGC kinase inhibitor balanol. The selectivity of balanol among human GRKs is assessed.
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===Human GRK2 in complex with Gbetgamma subunits and balanol (soak)===
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Structure of Human G Protein-Coupled Receptor Kinase 2 in Complex with the Kinase Inhibitor Balanol.,Tesmer JJ, Tesmer VM, Lodowski DT, Steinhagen H, Huber J J Med Chem. 2010 Feb 3. PMID:20128603<ref>PMID:20128603</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 3krw" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_20128603}}, adds the Publication Abstract to the page
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*[[Beta adrenergic receptor kinase 3D structures|Beta adrenergic receptor kinase 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 20128603 is the PubMed ID number.
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*[[Transducin 3D structures|Transducin 3D structures]]
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== References ==
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{{ABSTRACT_PUBMED_20128603}}
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<references/>
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__TOC__
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==About this Structure==
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</StructureSection>
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3KRW is a 3 chains structure with sequences from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] and [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3KRW OCA].
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==Reference==
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<ref group="xtra">PMID:20128603</ref><references group="xtra"/>
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[[Category: Bos taurus]]
[[Category: Bos taurus]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Tesmer, J J.G.]]
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[[Category: Large Structures]]
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[[Category: Tesmer, V M.]]
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[[Category: Tesmer JJG]]
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[[Category: Acetylation]]
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[[Category: Tesmer VM]]
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[[Category: Atp-binding]]
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[[Category: Cell membrane]]
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[[Category: Complex]]
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[[Category: Inhibitor]]
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[[Category: Kinase]]
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[[Category: Lipoprotein]]
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[[Category: Membrane]]
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[[Category: Methylation]]
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[[Category: Nucleotide-binding]]
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[[Category: Ph domain]]
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[[Category: Phosphoprotein]]
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[[Category: Polymorphism]]
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[[Category: Prenylation]]
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[[Category: Protein binding]]
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[[Category: Protein kinase]]
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[[Category: Rgs homology domain]]
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[[Category: Serine/threonine-protein kinase]]
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[[Category: Transducer]]
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[[Category: Transferase]]
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[[Category: Wd repeat]]
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[[Category: Wd40]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Feb 17 10:21:48 2010''
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Current revision

Human GRK2 in complex with Gbetgamma subunits and balanol (soak)

PDB ID 3krw

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