5l4q

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m (Protected "5l4q" [edit=sysop:move=sysop])
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'''Unreleased structure'''
 
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The entry 5l4q is ON HOLD
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==Crystal Structure of Adaptor Protein 2 Associated Kinase 1 (AAK1) in Complex with LKB1 (AAK1 Dual Inhibitor)==
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<StructureSection load='5l4q' size='340' side='right' caption='[[5l4q]], [[Resolution|resolution]] 1.97&Aring;' scene=''>
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Authors: Sorrell, F.J., Williams, E., Fox, N., Abdul Azeez, K.R., Gileadi, O., von Delft, F., Edwards, A.M., Bountra, C., Elkins, J.M., Knapp, S.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5l4q]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5L4Q OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5L4Q FirstGlance]. <br>
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Description: Crystal Structure of Adaptor Protein 2 Associated Kinase 1 (AAK1) in Complex with LKB1 (AAK1 Dual Inhibitor)
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=LKB:~{N}-[5-(4-CYANOPHENYL)-1~{H}-PYRROLO[2,3-B]PYRIDIN-3-YL]PYRIDINE-3-CARBOXAMIDE'>LKB</scene></td></tr>
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[[Category: Unreleased Structures]]
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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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[[Category: Elkins, J.M]]
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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=5l4q FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5l4q OCA], [http://pdbe.org/5l4q PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5l4q RCSB], [http://www.ebi.ac.uk/pdbsum/5l4q PDBsum]</span></td></tr>
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[[Category: Knapp, S]]
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</table>
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[[Category: Abdul Azeez, K.R]]
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== 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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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Non-specific serine/threonine protein kinase]]
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[[Category: Azeez, K R.Abdul]]
[[Category: Bountra, C]]
[[Category: Bountra, C]]
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[[Category: Sorrell, F.J]]
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[[Category: Delft, F von]]
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[[Category: Edwards, A M]]
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[[Category: Elkins, J M]]
[[Category: Fox, N]]
[[Category: Fox, N]]
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[[Category: Gileadi, O]]
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[[Category: Knapp, S]]
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[[Category: Sorrell, F J]]
[[Category: Williams, E]]
[[Category: Williams, E]]
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[[Category: Von Delft, F]]
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[[Category: Kinase kinase domain]]
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[[Category: Edwards, A.M]]
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[[Category: Transferase]]
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[[Category: Gileadi, O]]
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Revision as of 15:29, 20 June 2016

Crystal Structure of Adaptor Protein 2 Associated Kinase 1 (AAK1) in Complex with LKB1 (AAK1 Dual Inhibitor)

5l4q, resolution 1.97Å

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