4li5

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{{STRUCTURE_4li5| PDB=4li5 | SCENE= }}
 
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===EGFR-K IN COMPLEX WITH N-[3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]-4-methoxy-phenyl] Prop-2-enamide===
 
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{{ABSTRACT_PUBMED_23930994}}
 
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==Disease==
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==EGFR-K IN COMPLEX WITH N-[3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]-4-methoxy-phenyl] Prop-2-enamide==
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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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<StructureSection load='4li5' size='340' side='right'caption='[[4li5]], [[Resolution|resolution]] 2.64&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4li5]] 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=4LI5 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4LI5 FirstGlance]. <br>
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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]] 2.64&#8491;</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=1WY:N-(3-{[5-CHLORO-4-(1H-INDOL-3-YL)PYRIMIDIN-2-YL]AMINO}-4-METHOXYPHENYL)PROPANAMIDE'>1WY</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene></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=4li5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4li5 OCA], [https://pdbe.org/4li5 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4li5 RCSB], [https://www.ebi.ac.uk/pdbsum/4li5 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4li5 ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[https://www.uniprot.org/uniprot/EGFR_HUMAN EGFR_HUMAN] Defects in EGFR are associated with lung cancer (LNCR) [MIM:[https://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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[https://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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==Function==
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==See Also==
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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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*[[Epidermal growth factor receptor 3D structures|Epidermal growth factor receptor 3D structures]]
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== References ==
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==About this Structure==
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<references/>
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[[4li5]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4LI5 OCA].
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__TOC__
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</StructureSection>
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==Reference==
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<ref group="xtra">PMID:023930994</ref><references group="xtra"/><references/>
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Receptor protein-tyrosine kinase]]
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[[Category: Large Structures]]
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[[Category: Anderton, M.]]
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[[Category: Anderton M]]
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[[Category: Ashton, S.]]
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[[Category: Ashton S]]
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[[Category: Augustin, M.]]
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[[Category: Augustin M]]
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[[Category: Bethel, P.]]
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[[Category: Bethel P]]
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[[Category: Box, M.]]
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[[Category: Box M]]
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[[Category: Butterworth, S.]]
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[[Category: Butterworth S]]
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[[Category: Chroley, C.]]
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[[Category: Chroley C]]
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[[Category: Chuaqui, C.]]
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[[Category: Chuaqui C]]
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[[Category: Colclough, N.]]
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[[Category: Colclough N]]
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[[Category: Cross, D.]]
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[[Category: Cross D]]
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[[Category: Debreczeni, J E.]]
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[[Category: Debreczeni JE]]
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[[Category: Eberlein, C.]]
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[[Category: Eberlein C]]
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[[Category: Finlay, R.]]
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[[Category: Finlay R]]
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[[Category: Grist, M.]]
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[[Category: Grist M]]
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[[Category: Hill, G.]]
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[[Category: Hill G]]
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[[Category: Kiefersauer, R.]]
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[[Category: Kiefersauer R]]
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[[Category: Klinowska, T.]]
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[[Category: Klinowska T]]
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[[Category: Lane, C.]]
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[[Category: Lane C]]
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[[Category: Martin, S.]]
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[[Category: Martin S]]
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[[Category: Nagel, S.]]
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[[Category: Nagel S]]
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[[Category: Orme, J.]]
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[[Category: Orme J]]
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[[Category: Seiffert, G B.]]
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[[Category: Seiffert GB]]
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[[Category: Smith, P.]]
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[[Category: Smith P]]
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[[Category: Wang, F.]]
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[[Category: Wang F]]
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[[Category: Ward, R.]]
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[[Category: Ward R]]
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[[Category: Waring, M.]]
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[[Category: Waring M]]
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[[Category: Egf receptor kinase]]
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[[Category: Inhibitor]]
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[[Category: Transferase-transferase inhibitor complex]]
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Current revision

EGFR-K IN COMPLEX WITH N-[3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]-4-methoxy-phenyl] Prop-2-enamide

PDB ID 4li5

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