5j9z - Revision history

OCA at 10:56, 6 September 2023

OCA — Wed, 06 Sep 2023 10:56:22 GMT

←Older revision		Revision as of 10:56, 6 September 2023
Line 1:		Line 1:

	==EGFR-T790M in complex with pyrazolopyrimidine inhibitor 1a==		==EGFR-T790M in complex with pyrazolopyrimidine inhibitor 1a==
-	<StructureSection load='5j9z' size='340' side='right' caption='[[5j9z]], [[Resolution\|resolution]] 2.50Å' scene=''>	+	<StructureSection load='5j9z' size='340' side='right'caption='[[5j9z]], [[Resolution\|resolution]] 2.50Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5j9z]] is a 1 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/~~Human Human~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5J9Z OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5J9Z FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5j9z]] 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=5J9Z OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5J9Z FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6HJ:(R)-1-(3-(4-AMINO-3-(1-METHYL-1H-INDOL-3-YL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-1-YL)PIPERIDIN-1-YL)PROP-2-EN-1-ONE'>6HJ</scene~~></td></tr>~~	+	</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models\|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution\|Resolution]] 2.5Å</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">EGFR, ERBB, ERBB1, HER1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6HJ:(R)-1-(3-(4-AMINO-3-(1-METHYL-1H-INDOL-3-YL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-1-YL)PIPERIDIN-1-YL)PROP-2-EN-1-ONE'>6HJ</scene></td></tr>
-	<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>	+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5j9z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5j9z OCA], [https://pdbe.org/5j9z PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5j9z RCSB], [https://www.ebi.ac.uk/pdbsum/5j9z PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5j9z ProSAT]</span></td></tr>
-	<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=5j9z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5j9z OCA], [~~http~~://pdbe.org/5j9z PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5j9z RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5j9z PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5j9z ProSAT]</span></td></tr>	+
	</table>		</table>
	== Disease ==		== Disease ==
-	[~~[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.	+	[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.
	== Function ==		== Function ==
-	[~~[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>	+	[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>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 24:		Line 23:

	==See Also==		==See Also==
-	*[[Epidermal ~~Growth Factor Receptor~~\|Epidermal ~~Growth Factor Receptor~~]]	+	*[[Epidermal growth factor receptor 3D structures\|Epidermal growth factor receptor 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
-	[[Category: ~~Receptor protein-tyrosine kinase~~]]	+	[[Category: Large Structures]]
-	[[Category: Becker, C]]	+	[[Category: Becker C]]
-	[[Category: Engel, J]]	+	[[Category: Engel J]]
-	[[Category: Rauh, D]]	+	[[Category: Rauh D]]
-	~~[[Category: Covalent inhibitor]]~~	+
-	~~[[Category: Drug resistance]]~~	+
-	~~[[Category: Transferase]]~~	+
-	~~[[Category: Tyrosine kinase~~]]	+

OCA at 07:12, 21 February 2019

OCA — Thu, 21 Feb 2019 07:12:19 GMT

←Older revision		Revision as of 07:12, 21 February 2019
Line 3:		Line 3:
	<StructureSection load='5j9z' size='340' side='right' caption='[[5j9z]], [[Resolution\|resolution]] 2.50Å' scene=''>		<StructureSection load='5j9z' size='340' side='right' caption='[[5j9z]], [[Resolution\|resolution]] 2.50Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5j9z]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5J9Z OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5J9Z FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5j9z]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5J9Z OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5J9Z FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6HJ:(R)-1-(3-(4-AMINO-3-(1-METHYL-1H-INDOL-3-YL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-1-YL)PIPERIDIN-1-YL)PROP-2-EN-1-ONE'>6HJ</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6HJ:(R)-1-(3-(4-AMINO-3-(1-METHYL-1H-INDOL-3-YL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-1-YL)PIPERIDIN-1-YL)PROP-2-EN-1-ONE'>6HJ</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">EGFR, ERBB, ERBB1, HER1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
	<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>		<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>
	<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=5j9z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5j9z OCA], [http://pdbe.org/5j9z PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5j9z RCSB], [http://www.ebi.ac.uk/pdbsum/5j9z PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5j9z ProSAT]</span></td></tr>		<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=5j9z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5j9z OCA], [http://pdbe.org/5j9z PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5j9z RCSB], [http://www.ebi.ac.uk/pdbsum/5j9z PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5j9z ProSAT]</span></td></tr>
Line 21:		Line 22:
	</div>		</div>
	<div class="pdbe-citations 5j9z" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 5j9z" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Epidermal Growth Factor Receptor\|Epidermal Growth Factor Receptor]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]
	[[Category: Becker, C]]		[[Category: Becker, C]]

OCA at 00:05, 10 September 2016

OCA — Sat, 10 Sep 2016 00:05:33 GMT

←Older revision		Revision as of 00:05, 10 September 2016
Line 4:		Line 4:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[5j9z]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5J9Z OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5J9Z FirstGlance]. <br>		<table><tr><td colspan='2'>[[5j9z]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5J9Z OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5J9Z FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6HJ:(R)-1-(3-(4-~~amino~~-3-(1-~~methyl~~-1H-~~indol~~-3-yl)-1H-~~pyrazolo~~[3,4-d]~~pyrimidin~~-1-yl)~~piperidin~~-1-yl)~~prop~~-2-en-1-~~one~~'>6HJ</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6HJ:(R)-1-(3-(4-AMINO-3-(1-METHYL-1H-INDOL-3-YL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-1-YL)PIPERIDIN-1-YL)PROP-2-EN-1-ONE'>6HJ</scene></td></tr>
	<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>		<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>
	<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=5j9z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5j9z OCA], [http://pdbe.org/5j9z PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5j9z RCSB], [http://www.ebi.ac.uk/pdbsum/5j9z PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5j9z ProSAT]</span></td></tr>		<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=5j9z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5j9z OCA], [http://pdbe.org/5j9z PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5j9z RCSB], [http://www.ebi.ac.uk/pdbsum/5j9z PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5j9z ProSAT]</span></td></tr>

OCA at 04:54, 9 September 2016

OCA — Fri, 09 Sep 2016 04:54:52 GMT

←Older revision		Revision as of 04:54, 9 September 2016
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 5j9z is ~~ON HOLD~~ ~~until Apr 11 2018~~	+	==EGFR-T790M in complex with pyrazolopyrimidine inhibitor 1a==
		+	<StructureSection load='5j9z' size='340' side='right' caption='[[5j9z]], [[Resolution\|resolution]] 2.50Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[5j9z]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5J9Z OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5J9Z FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6HJ:(R)-1-(3-(4-amino-3-(1-methyl-1H-indol-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one'>6HJ</scene></td></tr>
		+	<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>
		+	<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=5j9z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5j9z OCA], [http://pdbe.org/5j9z PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5j9z RCSB], [http://www.ebi.ac.uk/pdbsum/5j9z PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5j9z ProSAT]</span></td></tr>
		+	</table>
		+	== Disease ==
		+	[[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.
		+	== Function ==
		+	[[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>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Targeting acquired drug resistance represents the major challenge in the treatment of EGFR-driven non-small-cell lung cancer (NSCLC). Herein, we describe the structure-based design, synthesis, and biological evaluation of a novel class of covalent EGFR inhibitors that exhibit excellent inhibition of EGFR-mutant drug-resistant cells. Protein X-ray crystallography combined with detailed kinetic studies led to a deeper understanding of the mode of inhibition of EGFR-T790M and provided insight into the key principles for effective inhibition of the recently discovered tertiary mutation at EGFR-C797S.

-	~~Authors~~:	+	Insight into the Inhibition of Drug-Resistant Mutants of the Receptor Tyrosine Kinase EGFR.,Engel J, Becker C, Lategahn J, Keul M, Ketzer J, Muhlenberg T, Kollipara L, Schultz-Fademrecht C, Zahedi RP, Bauer S, Rauh D Angew Chem Int Ed Engl. 2016 Aug 26;55(36):10909-12. doi: 10.1002/anie.201605011., Epub 2016 Aug 5. PMID:27496389<ref>PMID:27496389</ref>

-	~~Description~~:	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased Structures~~]]	+	</div>
		+	<div class="pdbe-citations 5j9z" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Receptor protein-tyrosine kinase]]
		+	[[Category: Becker, C]]
		+	[[Category: Engel, J]]
		+	[[Category: Rauh, D]]
		+	[[Category: Covalent inhibitor]]
		+	[[Category: Drug resistance]]
		+	[[Category: Transferase]]
		+	[[Category: Tyrosine kinase]]

OCA at 15:12, 15 May 2016

OCA — Sun, 15 May 2016 15:12:42 GMT

←Older revision		Revision as of 15:12, 15 May 2016
Line 3:		Line 3:
	The entry 5j9z is ON HOLD until Apr 11 2018		The entry 5j9z is ON HOLD until Apr 11 2018

-	Authors: ~~Becker, C., Engel, J., Rauh, D.~~	+	Authors:

	Description:		Description:
	[[Category: Unreleased Structures]]		[[Category: Unreleased Structures]]
-	[[Category: Rauh, D]]
-	[[Category: Engel, J]]
-	[[Category: Becker, C]]

OCA: Protected "5j9z" [edit=sysop:move=sysop]

OCA — Wed, 11 May 2016 01:44:27 GMT

Protected "5j9z" [edit=sysop:move=sysop]

←Older revision

Revision as of 01:44, 11 May 2016

OCA: New page: '''Unreleased structure''' The entry 5j9z is ON HOLD until Apr 11 2018 Authors: Becker, C., Engel, J., Rauh, D. Description: Category: Unreleased Structures Category: Rauh, D ...

OCA — Wed, 11 May 2016 01:44:26 GMT

New page: '''Unreleased structure''' The entry 5j9z is ON HOLD until Apr 11 2018 Authors: Becker, C., Engel, J., Rauh, D. Description: Category: Unreleased Structures Category: Rauh, D ...

New page

'''Unreleased structure'''

The entry 5j9z is ON HOLD until Apr 11 2018

Authors: Becker, C., Engel, J., Rauh, D.

Description:
[[Category: Unreleased Structures]]
[[Category: Rauh, D]]
[[Category: Engel, J]]
[[Category: Becker, C]]