3qc9: Difference between revisions

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[[Image:3qc9.png|left|200px]]
==Crystal structure of cross-linked bovine GRK1 T8C/N480C double mutant complexed with ADP and Mg==
<StructureSection load='3qc9' size='340' side='right' caption='[[3qc9]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[3qc9]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QC9 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3QC9 FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ADP:ADENOSINE-5-DIPHOSPHATE'>ADP</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">GRK1, RHOK ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 Bos taurus])</td></tr>
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Rhodopsin_kinase Rhodopsin kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.14 2.7.11.14] </span></td></tr>
<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=3qc9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qc9 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3qc9 RCSB], [http://www.ebi.ac.uk/pdbsum/3qc9 PDBsum]</span></td></tr>
</table>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
G protein-coupled receptor kinases (GRKs) phosphorylate activated G protein-coupled receptors (GPCRs) to initiate receptor desensitization. In addition to the canonical phosphoacceptor site of the kinase domain, activated receptors bind to a distinct docking site that confers higher affinity and activates GRKs allosterically. Recent mutagenesis and structural studies support a model wherein receptor docking activates a GRK by stabilizing the interaction of its ~20 amino acid N-terminal region with the kinase domain. This interaction in turn stabilizes a closed, more active conformation of the enzyme. To investigate the importance of this interaction for the process of GRK activation, we first validated the functionality of the N-terminal region in rhodopsin kinase (GRK1) by site-directed mutagenesis and then introduced a disulfide bond to cross-link the N-terminal region of GRK1 with its specific binding site on the kinase domain. Characterization of the kinetic and biophysical properties of the cross-linked protein showed that disulfide bond formation greatly enhances the catalytic efficiency of the peptide phosphorylation, but receptor-dependent phosphorylation, Meta II stabilization, and inhibition of transducin activation were unaffected. These data indicate that the interaction of the N-terminal region with the kinase domain is important for GRK activation, but that it does not dictate the affinity of GRKs for activated receptors.


{{STRUCTURE_3qc9|  PDB=3qc9  |  SCENE=  }}
Activation of G protein-coupled receptor kinase 1 involves interactions between its N-terminal region and its kinase domain.,Huang CC, Orban T, Jastrzebska B, Palczewski K, Tesmer JJ Biochemistry. 2011 Jan 25. PMID:21265573<ref>PMID:21265573</ref>


===Crystal structure of cross-linked bovine GRK1 T8C/N480C double mutant complexed with ADP and Mg===
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
 
</div>
{{ABSTRACT_PUBMED_21265573}}
 
==About this Structure==
[[3qc9]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QC9 OCA].


==See Also==
==See Also==
*[[Rhodopsin|Rhodopsin]]
*[[Rhodopsin|Rhodopsin]]
 
== References ==
==Reference==
<references/>
<ref group="xtra">PMID:021265573</ref><references group="xtra"/>
__TOC__
</StructureSection>
[[Category: Bos taurus]]
[[Category: Bos taurus]]
[[Category: Rhodopsin kinase]]
[[Category: Rhodopsin kinase]]
[[Category: Huang, C C.]]
[[Category: Huang, C C]]
[[Category: Tesmer, J J.G.]]
[[Category: Tesmer, J J.G]]
[[Category: Enkaryotic protein kinase fold]]
[[Category: Enkaryotic protein kinase fold]]
[[Category: Protein serine/threonine kinase]]
[[Category: Protein serine/threonine kinase]]
[[Category: Transferase]]
[[Category: Transferase]]
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