5d41

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'''Unreleased structure'''
 
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The entry 5d41 is ON HOLD until Paper Publication
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==EGFR kinase domain in complex with mutant selective allosteric inhibitor==
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<StructureSection load='5d41' size='340' side='right' caption='[[5d41]], [[Resolution|resolution]] 2.31&Aring;' scene=''>
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Authors: Yun, C.-H., Park, E., Eck, M.J.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[5d41]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5D41 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5D41 FirstGlance]. <br>
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Description: EGFR kinase domain in complex with mutant selective allosteric inhibitor
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=57N:(2R)-2-(1-OXO-1,3-DIHYDRO-2H-ISOINDOL-2-YL)-2-PHENYL-N-(1,3-THIAZOL-2-YL)ACETAMIDE'>57N</scene>, <scene name='pdbligand=ANP:PHOSPHOAMINOPHOSPHONIC+ACID-ADENYLATE+ESTER'>ANP</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</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/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1] </span></td></tr>
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[[Category: Yun, C.-H]]
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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=5d41 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5d41 OCA], [http://pdbe.org/5d41 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5d41 RCSB], [http://www.ebi.ac.uk/pdbsum/5d41 PDBsum]</span></td></tr>
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[[Category: Eck, M.J]]
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</table>
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== Disease ==
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[[http://www.uniprot.org/uniprot/EGFR_HUMAN EGFR_HUMAN]] Defects in EGFR are associated with lung cancer (LNCR) [MIM:[http://omim.org/entry/211980 211980]]. LNCR is a common malignancy affecting tissues of the lung. The most common form of lung cancer is non-small cell lung cancer (NSCLC) that can be divided into 3 major histologic subtypes: squamous cell carcinoma, adenocarcinoma, and large cell lung cancer. NSCLC is often diagnosed at an advanced stage and has a poor prognosis.
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== Function ==
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[[http://www.uniprot.org/uniprot/EGFR_HUMAN EGFR_HUMAN]] Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses. Known ligands include EGF, TGFA/TGF-alpha, amphiregulin, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF. Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on key cytoplasmic residues. The phosphorylated receptor recruits adapter proteins like GRB2 which in turn activates complex downstream signaling cascades. Activates at least 4 major downstream signaling cascades including the RAS-RAF-MEK-ERK, PI3 kinase-AKT, PLCgamma-PKC and STATs modules. May also activate the NF-kappa-B signaling cascade. Also directly phosphorylates other proteins like RGS16, activating its GTPase activity and probably coupling the EGF receptor signaling to the G protein-coupled receptor signaling. Also phosphorylates MUC1 and increases its interaction with SRC and CTNNB1/beta-catenin.<ref>PMID:7657591</ref> <ref>PMID:11602604</ref> <ref>PMID:12873986</ref> <ref>PMID:10805725</ref> <ref>PMID:11116146</ref> <ref>PMID:11483589</ref> <ref>PMID:17115032</ref> <ref>PMID:21258366</ref> <ref>PMID:12297050</ref> <ref>PMID:12620237</ref> <ref>PMID:15374980</ref> <ref>PMID:19560417</ref> <ref>PMID:20837704</ref> Isoform 2 may act as an antagonist of EGF action.<ref>PMID:7657591</ref> <ref>PMID:11602604</ref> <ref>PMID:12873986</ref> <ref>PMID:10805725</ref> <ref>PMID:11116146</ref> <ref>PMID:11483589</ref> <ref>PMID:17115032</ref> <ref>PMID:21258366</ref> <ref>PMID:12297050</ref> <ref>PMID:12620237</ref> <ref>PMID:15374980</ref> <ref>PMID:19560417</ref> <ref>PMID:20837704</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: Receptor protein-tyrosine kinase]]
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[[Category: Eck, M J]]
[[Category: Park, E]]
[[Category: Park, E]]
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[[Category: Yun, C H]]
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[[Category: Allosteric inhibitor]]
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[[Category: Egfr]]
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[[Category: Transferase-transferase inhibitor complex]]

Revision as of 15:20, 20 June 2016

EGFR kinase domain in complex with mutant selective allosteric inhibitor

5d41, resolution 2.31Å

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