5te0

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<StructureSection load='5te0' size='340' side='right'caption='[[5te0]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
<StructureSection load='5te0' size='340' side='right'caption='[[5te0]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[5te0]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5TE0 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5TE0 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[5te0]] 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=5TE0 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5TE0 FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene>, <scene name='pdbligand=XIN:METHYL+(3Z)-3-{[(4-{METHYL[(4-METHYLPIPERAZIN-1-YL)ACETYL]AMINO}PHENYL)AMINO](PHENYL)METHYLIDENE}-2-OXO-2,3-DIHYDRO-1H-INDOLE-6-CARBOXYLATE'>XIN</scene></td></tr>
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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]] 1.9&#8491;</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">AAK1, KIAA1048 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene>, <scene name='pdbligand=XIN:METHYL+(3Z)-3-{[(4-{METHYL[(4-METHYLPIPERAZIN-1-YL)ACETYL]AMINO}PHENYL)AMINO](PHENYL)METHYLIDENE}-2-OXO-2,3-DIHYDRO-1H-INDOLE-6-CARBOXYLATE'>XIN</scene></td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span></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=5te0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5te0 OCA], [https://pdbe.org/5te0 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5te0 RCSB], [https://www.ebi.ac.uk/pdbsum/5te0 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5te0 ProSAT]</span></td></tr>
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<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=5te0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5te0 OCA], [http://pdbe.org/5te0 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5te0 RCSB], [http://www.ebi.ac.uk/pdbsum/5te0 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5te0 ProSAT]</span></td></tr>
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</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/AAK1_HUMAN AAK1_HUMAN]] Regulates clathrin-mediated endocytosis by phosphorylating the AP2M1/mu2 subunit of the adaptor protein complex 2 (AP-2) which ensures high affinity binding of AP-2 to cargo membrane proteins during the initial stages of endocytosis. Isoform 1 and isoform 2 display similar levels of kinase activity towards AP2M1. Regulates phosphorylation of other AP-2 subunits as well as AP-2 localization and AP-2-mediated internalization of ligand complexes. Phosphorylates NUMB and regulates its cellular localization, promoting NUMB localization to endosomes. Binds to and stabilizes the activated form of NOTCH1, increases its localization in endosomes and regulates its transcriptional activity.<ref>PMID:12952931</ref> <ref>PMID:17494869</ref> <ref>PMID:18657069</ref> <ref>PMID:21464124</ref>
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[https://www.uniprot.org/uniprot/AAK1_HUMAN AAK1_HUMAN] Regulates clathrin-mediated endocytosis by phosphorylating the AP2M1/mu2 subunit of the adaptor protein complex 2 (AP-2) which ensures high affinity binding of AP-2 to cargo membrane proteins during the initial stages of endocytosis. Isoform 1 and isoform 2 display similar levels of kinase activity towards AP2M1. Regulates phosphorylation of other AP-2 subunits as well as AP-2 localization and AP-2-mediated internalization of ligand complexes. Phosphorylates NUMB and regulates its cellular localization, promoting NUMB localization to endosomes. Binds to and stabilizes the activated form of NOTCH1, increases its localization in endosomes and regulates its transcriptional activity.<ref>PMID:12952931</ref> <ref>PMID:17494869</ref> <ref>PMID:18657069</ref> <ref>PMID:21464124</ref>
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
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[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Non-specific serine/threonine protein kinase]]
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[[Category: Arruda P]]
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[[Category: Arruda, P]]
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[[Category: Bountra C]]
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[[Category: Bountra, C]]
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[[Category: Counago RM]]
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[[Category: Counago, R M]]
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[[Category: Edwards AM]]
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[[Category: Edwards, A M]]
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[[Category: Elkins JM]]
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[[Category: Elkins, J M]]
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[[Category: Gileadi O]]
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[[Category: Gileadi, O]]
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[[Category: Structural genomic]]
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[[Category: Protein kinase domain]]
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[[Category: Sgc]]
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[[Category: Transferase]]
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[[Category: Transferase-transferase inhibitor complex]]
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Current revision

Crystal Structure of Adaptor Protein 2 Associated Kinase (AAK1) in complex with BIBF 1120

PDB ID 5te0

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Proteopedia Page Contributors and Editors (what is this?)

OCA

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