7a6i - Revision history

OCA at 12:04, 1 February 2024

2024-02-01T12:04:22Z

←Older revision		Revision as of 12:04, 1 February 2024
Line 1:		Line 1:

	==Crystal Structure of EGFR-T790M/V948R in Complex with LDC8201==		==Crystal Structure of EGFR-T790M/V948R in Complex with LDC8201==
-	<StructureSection load='7a6i' size='340' side='right'caption='[[7a6i]]' scene=''>	+	<StructureSection load='7a6i' size='340' side='right'caption='[[7a6i]], [[Resolution\|resolution]] 2.40Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7A6I OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7A6I FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[7a6i]] 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=7A6I OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7A6I FirstGlance]. <br>
-	</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=7a6i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7a6i OCA], [https://pdbe.org/7a6i PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7a6i RCSB], [https://www.ebi.ac.uk/pdbsum/7a6i PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7a6i ProSAT]</span></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]] 2.4Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=R1W:~{N}-[5-[4-chloranyl-2-[4-(4-methylpiperazin-1-yl)phenyl]-1~{H}-pyrrolo[2,3-b]pyridin-3-yl]-2-methyl-phenyl]propanamide'>R1W</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></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=7a6i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7a6i OCA], [https://pdbe.org/7a6i PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7a6i RCSB], [https://www.ebi.ac.uk/pdbsum/7a6i PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7a6i ProSAT]</span></td></tr>
	</table>		</table>
		+	== Disease ==
		+	[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 ==
		+	[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;">
		+	== Publication Abstract from PubMed ==
		+	Despite the clinical efficacy of epidermal growth factor receptor (EGFR) inhibitors, a subset of patients with non-small cell lung cancer displays insertion mutations in exon20 in EGFR and Her2 with limited treatment options. Here, we present the development and characterization of the novel covalent inhibitors LDC8201 and LDC0496 based on a 1H-pyrrolo[2,3-b]pyridine scaffold. They exhibited intense inhibitory potency toward EGFR and Her2 exon20 insertion mutations as well as selectivity over wild type EGFR and within the kinome. Complex crystal structures with the inhibitors and biochemical and cellular on-target activity document their favorable binding characteristics. Ultimately, we observed tumor shrinkage in mice engrafted with patient-derived EGFR-H773_V774insNPH mutant cells during treatment with LDC8201. Together, these results highlight the potential of covalent pyrrolopyridines as inhibitors to target exon20 insertion mutations.
		+
		+	Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors.,Lategahn J, Tumbrink HL, Schultz-Fademrecht C, Heimsoeth A, Werr L, Niggenaber J, Keul M, Parmaksiz F, Baumann M, Menninger S, Zent E, Landel I, Weisner J, Jeyakumar K, Heyden L, Russ N, Muller F, Lorenz C, Bragelmann J, Spille I, Grabe T, Muller MP, Heuckmann JM, Klebl BM, Nussbaumer P, Sos ML, Rauh D J Med Chem. 2022 Apr 29. doi: 10.1021/acs.jmedchem.1c02080. PMID:35486541<ref>PMID:35486541</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 7a6i" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Epidermal growth factor receptor 3D structures\|Epidermal growth factor receptor 3D structures]]
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: Mueller MP]]		[[Category: Mueller MP]]
	[[Category: Niggenaber J]]		[[Category: Niggenaber J]]
	[[Category: Rauh D]]		[[Category: Rauh D]]

OCA at 14:42, 31 August 2022

2022-08-31T14:42:35Z

←Older revision		Revision as of 14:42, 31 August 2022
Line 1:		Line 1:

	==Crystal Structure of EGFR-T790M/V948R in Complex with LDC8201==		==Crystal Structure of EGFR-T790M/V948R in Complex with LDC8201==
-	<StructureSection load='7a6i' size='340' side='right'caption='[[7a6i]]~~, [[Resolution\|resolution]] 2.40Å~~' scene=''>	+	<StructureSection load='7a6i' size='340' side='right'caption='[[7a6i]]' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>~~[[7a6i]] is a 1 chain structure.~~ Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7A6I OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7A6I FirstGlance]. <br>	+	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7A6I OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7A6I FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=R1W:~{N}-[5-[4-chloranyl-2-[4-(4-methylpiperazin-1-yl)phenyl]-1~{H}-pyrrolo[2,3-b]pyridin-3-yl]-2-methyl-phenyl]propanamide'>R1W</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>	+	</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=7a6i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7a6i OCA], [https://pdbe.org/7a6i PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7a6i RCSB], [https://www.ebi.ac.uk/pdbsum/7a6i PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7a6i ProSAT]</span></td></tr>
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [https://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=7a6i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7a6i OCA], [https://pdbe.org/7a6i PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7a6i RCSB], [https://www.ebi.ac.uk/pdbsum/7a6i PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7a6i ProSAT]</span></td></tr>	+
	</table>		</table>
-	== Disease ==
-	[[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 ==
-	[[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;">
-	== Publication Abstract from PubMed ==
-	Despite the clinical efficacy of epidermal growth factor receptor (EGFR) inhibitors, a subset of patients with non-small cell lung cancer displays insertion mutations in exon20 in EGFR and Her2 with limited treatment options. Here, we present the development and characterization of the novel covalent inhibitors LDC8201 and LDC0496 based on a 1H-pyrrolo[2,3-b]pyridine scaffold. They exhibited intense inhibitory potency toward EGFR and Her2 exon20 insertion mutations as well as selectivity over wild type EGFR and within the kinome. Complex crystal structures with the inhibitors and biochemical and cellular on-target activity document their favorable binding characteristics. Ultimately, we observed tumor shrinkage in mice engrafted with patient-derived EGFR-H773_V774insNPH mutant cells during treatment with LDC8201. Together, these results highlight the potential of covalent pyrrolopyridines as inhibitors to target exon20 insertion mutations.
-
-	Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors.,Lategahn J, Tumbrink HL, Schultz-Fademrecht C, Heimsoeth A, Werr L, Niggenaber J, Keul M, Parmaksiz F, Baumann M, Menninger S, Zent E, Landel I, Weisner J, Jeyakumar K, Heyden L, Russ N, Muller F, Lorenz C, Bragelmann J, Spille I, Grabe T, Muller MP, Heuckmann JM, Klebl BM, Nussbaumer P, Sos ML, Rauh D J Med Chem. 2022 Apr 29. doi: 10.1021/acs.jmedchem.1c02080. PMID:35486541<ref>PMID:35486541</ref>
-
-	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	</div>
-	<div class="pdbe-citations 7a6i" style="background-color:#fffaf0;"></div>
-	== References ==
-	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	~~[[Category: Receptor protein-tyrosine kinase]]~~	+	[[Category: Mueller MP]]
-	[[Category: Mueller~~, M P~~]]	+	[[Category: Niggenaber J]]
-	[[Category: Niggenaber, J]]	+	[[Category: Rauh D]]
-	[[Category: Rauh, D]]	+
-	~~[[Category: Covalent]]~~	+
-	~~[[Category: Egfr]]~~	+
-	~~[[Category: Exon20]]~~	+
-	~~[[Category: T790m/v948r]]~~	+
-	~~[[Category: Transferase~~]]	+

OCA at 06:24, 12 May 2022

2022-05-12T06:24:20Z

←Older revision		Revision as of 06:24, 12 May 2022
Line 1:		Line 1:

	==Crystal Structure of EGFR-T790M/V948R in Complex with LDC8201==		==Crystal Structure of EGFR-T790M/V948R in Complex with LDC8201==
-	<StructureSection load='7a6i' size='340' side='right'caption='[[7a6i]]' scene=''>	+	<StructureSection load='7a6i' size='340' side='right'caption='[[7a6i]], [[Resolution\|resolution]] 2.40Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7A6I OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7A6I FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[7a6i]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7A6I OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7A6I FirstGlance]. <br>
-	</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=7a6i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7a6i OCA], [https://pdbe.org/7a6i PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7a6i RCSB], [https://www.ebi.ac.uk/pdbsum/7a6i PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7a6i ProSAT]</span></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=R1W:~{N}-[5-[4-chloranyl-2-[4-(4-methylpiperazin-1-yl)phenyl]-1~{H}-pyrrolo[2,3-b]pyridin-3-yl]-2-methyl-phenyl]propanamide'>R1W</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
		+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [https://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=7a6i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7a6i OCA], [https://pdbe.org/7a6i PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7a6i RCSB], [https://www.ebi.ac.uk/pdbsum/7a6i PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7a6i ProSAT]</span></td></tr>
	</table>		</table>
		+	== Disease ==
		+	[[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 ==
		+	[[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;">
		+	== Publication Abstract from PubMed ==
		+	Despite the clinical efficacy of epidermal growth factor receptor (EGFR) inhibitors, a subset of patients with non-small cell lung cancer displays insertion mutations in exon20 in EGFR and Her2 with limited treatment options. Here, we present the development and characterization of the novel covalent inhibitors LDC8201 and LDC0496 based on a 1H-pyrrolo[2,3-b]pyridine scaffold. They exhibited intense inhibitory potency toward EGFR and Her2 exon20 insertion mutations as well as selectivity over wild type EGFR and within the kinome. Complex crystal structures with the inhibitors and biochemical and cellular on-target activity document their favorable binding characteristics. Ultimately, we observed tumor shrinkage in mice engrafted with patient-derived EGFR-H773_V774insNPH mutant cells during treatment with LDC8201. Together, these results highlight the potential of covalent pyrrolopyridines as inhibitors to target exon20 insertion mutations.
		+
		+	Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors.,Lategahn J, Tumbrink HL, Schultz-Fademrecht C, Heimsoeth A, Werr L, Niggenaber J, Keul M, Parmaksiz F, Baumann M, Menninger S, Zent E, Landel I, Weisner J, Jeyakumar K, Heyden L, Russ N, Muller F, Lorenz C, Bragelmann J, Spille I, Grabe T, Muller MP, Heuckmann JM, Klebl BM, Nussbaumer P, Sos ML, Rauh D J Med Chem. 2022 Apr 29. doi: 10.1021/acs.jmedchem.1c02080. PMID:35486541<ref>PMID:35486541</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 7a6i" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Mueller MP]]	+	[[Category: Receptor protein-tyrosine kinase]]
-	[[Category: Niggenaber J]]	+	[[Category: Mueller, M P]]
-	[[Category: Rauh D]]	+	[[Category: Niggenaber, J]]
		+	[[Category: Rauh, D]]
		+	[[Category: Covalent]]
		+	[[Category: Egfr]]
		+	[[Category: Exon20]]
		+	[[Category: T790m/v948r]]
		+	[[Category: Transferase]]

OCA at 07:40, 23 February 2022

2022-02-23T07:40:19Z

←Older revision		Revision as of 07:40, 23 February 2022
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 7a6i ~~is ON HOLD until Paper Publication~~	+	==Crystal Structure of EGFR-T790M/V948R in Complex with LDC8201==
-		+	<StructureSection load='7a6i' size='340' side='right'caption='[[7a6i]]' scene=''>
-	~~Authors~~: ~~Niggenaber~~, J., ~~Mueller~~, M.P., ~~Rauh~~, D.	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7A6I OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7A6I FirstGlance]. <br>
-	~~Description: EGFR~~	+	</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=7a6i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7a6i OCA], [https://pdbe.org/7a6i PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7a6i RCSB], [https://www.ebi.ac.uk/pdbsum/7a6i PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7a6i ProSAT]</span></td></tr>
-	[[Category: ~~Unreleased~~ Structures]]	+	</table>
-	[[Category: Mueller~~, M.P~~]]	+	__TOC__
-	[[Category: ~~Rauh, D~~]]	+	</StructureSection>
-	[[Category: ~~Niggenaber, J~~]]	+	[[Category: Large Structures]]
		+	[[Category: Mueller MP]]
		+	[[Category: Niggenaber J]]
		+	[[Category: Rauh D]]

OCA: Protected "7a6i" [edit=sysop:move=sysop]

2020-09-02T05:05:48Z

Protected "7a6i" [edit=sysop:move=sysop]

←Older revision

Revision as of 05:05, 2 September 2020

OCA: New page: '''Unreleased structure''' The entry 7a6i is ON HOLD until Paper Publication Authors: Niggenaber, J., Mueller, M.P., Rauh, D. Description: EGFR Category: Unreleased Structures [[Ca...

2020-09-02T05:05:46Z

New page: '''Unreleased structure''' The entry 7a6i is ON HOLD until Paper Publication Authors: Niggenaber, J., Mueller, M.P., Rauh, D. Description: EGFR Category: Unreleased Structures [[Ca...

New page

'''Unreleased structure'''

The entry 7a6i is ON HOLD until Paper Publication

Authors: Niggenaber, J., Mueller, M.P., Rauh, D.

Description: EGFR
[[Category: Unreleased Structures]]
[[Category: Mueller, M.P]]
[[Category: Rauh, D]]
[[Category: Niggenaber, J]]