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5te0
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==Crystal Structure of Adaptor Protein 2 Associated Kinase (AAK1) in complex with BIBF 1120== | ==Crystal Structure of Adaptor Protein 2 Associated Kinase (AAK1) in complex with BIBF 1120== | ||
| - | <StructureSection load='5te0' size='340' side='right' caption='[[5te0]], [[Resolution|resolution]] 1.90Å' scene=''> | + | <StructureSection load='5te0' size='340' side='right'caption='[[5te0]], [[Resolution|resolution]] 1.90Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[5te0]] is a 1 chain structure. 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 [ | + | <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> |
| - | </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><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.9Å</td></tr> |
| - | + | <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> | |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | <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> |
</table> | </table> | ||
== Function == | == Function == | ||
| - | [ | + | [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> | ||
| - | [[Category: | + | [[Category: Homo sapiens]] |
| - | [[Category: Arruda | + | [[Category: Large Structures]] |
| - | [[Category: Bountra | + | [[Category: Arruda P]] |
| - | [[Category: Counago | + | [[Category: Bountra C]] |
| - | [[Category: Edwards | + | [[Category: Counago RM]] |
| - | [[Category: Elkins | + | [[Category: Edwards AM]] |
| - | [[Category: Gileadi | + | [[Category: Elkins JM]] |
| - | + | [[Category: Gileadi O]] | |
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Current revision
Crystal Structure of Adaptor Protein 2 Associated Kinase (AAK1) in complex with BIBF 1120
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