4mk0

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{{STRUCTURE_4mk0| PDB=4mk0 | SCENE= }}
 
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===Crystal structure of G protein-coupled receptor kinase 2 in complex with a a rationally designed paroxetine derivative===
 
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{{ABSTRACT_PUBMED_24220010}}
 
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==Function==
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==Crystal structure of G protein-coupled receptor kinase 2 in complex with a a rationally designed paroxetine derivative==
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[[http://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> [[http://www.uniprot.org/uniprot/GBG2_BOVIN GBG2_BOVIN]] Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction. [[http://www.uniprot.org/uniprot/GBB1_BOVIN GBB1_BOVIN]] Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction.
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<StructureSection load='4mk0' size='340' side='right'caption='[[4mk0]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4mk0]] 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=4MK0 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4MK0 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]] 2.4&#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=29X:5-{[(3S,4R)-4-(4-FLUOROPHENYL)PIPERIDIN-3-YL]METHOXY}-1H-ISOINDOL-1-ONE'>29X</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr>
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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=4mk0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4mk0 OCA], [https://pdbe.org/4mk0 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4mk0 RCSB], [https://www.ebi.ac.uk/pdbsum/4mk0 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4mk0 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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==About this Structure==
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==See Also==
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[[4mk0]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4MK0 OCA].
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*[[Beta adrenergic receptor kinase 3D structures|Beta adrenergic receptor kinase 3D structures]]
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*[[Transducin 3D structures|Transducin 3D structures]]
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==Reference==
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== References ==
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<ref group="xtra">PMID:024220010</ref><references group="xtra"/><references/>
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<references/>
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[[Category: Homan, K T.]]
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__TOC__
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[[Category: Tesmer, J J.G.]]
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</StructureSection>
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[[Category: Atp binding]]
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[[Category: Bos taurus]]
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[[Category: Hydrolase]]
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[[Category: Homo sapiens]]
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[[Category: Inhibitor complex]]
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[[Category: Large Structures]]
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[[Category: Peripheral membrane protein]]
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[[Category: Homan KT]]
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[[Category: Phosphorylation]]
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[[Category: Tesmer JJG]]
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[[Category: Protein kinase]]
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[[Category: Signaling protein-inhibitor complex]]
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Current revision

Crystal structure of G protein-coupled receptor kinase 2 in complex with a a rationally designed paroxetine derivative

PDB ID 4mk0

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