4wd5

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'''Unreleased structure'''
 
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The entry 4wd5 is ON HOLD until Paper Publication
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==Crystal structure of EGFR 696-1022 T790M in complex with QL-X138==
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<StructureSection load='4wd5' size='340' side='right' caption='[[4wd5]], [[Resolution|resolution]] 3.30&Aring;' scene=''>
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Authors: Yun, C.H., Eck, M.J.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4wd5]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4WD5 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4WD5 FirstGlance]. <br>
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Description: Crystal structure of EGFR 696-1022 T790M in complex with QL-X138
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3LH:N-{2-METHYL-5-[2-OXO-9-(1H-PYRAZOL-4-YL)BENZO[H][1,6]NAPHTHYRIDIN-1(2H)-YL]PHENYL}PROPANAMIDE'>3LH</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</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=4wd5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4wd5 OCA], [http://pdbe.org/4wd5 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4wd5 RCSB], [http://www.ebi.ac.uk/pdbsum/4wd5 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]]
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[[Category: Yun, C H]]
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[[Category: Egfr]]
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[[Category: Gatekeeper mutation]]
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[[Category: Inhibitor]]
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[[Category: T790m]]
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[[Category: Transferase-inhibitor complex]]

Revision as of 19:32, 13 May 2016

Crystal structure of EGFR 696-1022 T790M in complex with QL-X138

4wd5, resolution 3.30Å

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