5i9v - Revision history

OCA at 13:42, 30 August 2023

2023-08-30T13:42:56Z

←Older revision		Revision as of 13:42, 30 August 2023
Line 3:		Line 3:
	<StructureSection load='5i9v' size='340' side='right'caption='[[5i9v]], [[Resolution\|resolution]] 1.46Å' scene=''>		<StructureSection load='5i9v' size='340' side='right'caption='[[5i9v]], [[Resolution\|resolution]] 1.46Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5i9v]] 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=5I9V OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5I9V FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5i9v]] 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=5I9V OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5I9V FirstGlance]. <br>
-	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat"~~><scene name='pdbligand=AGS:PHOSPHOTHIOPHOSPHORIC+ACID-ADENYLATE+ESTER'>AGS</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]] 1.458Å</td></tr>
-	~~<tr~~ id~~='gene'><td class~~="~~sblockLbl~~">~~<b>~~[[~~Gene~~\|~~Gene:~~]]~~</b></td><td class="sblockDat">EPHA2, ECK ([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=AGS:PHOSPHOTHIOPHOSPHORIC+ACID-ADENYLATE+ESTER'>AGS</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=5i9v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5i9v OCA], [https://pdbe.org/5i9v PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5i9v RCSB], [https://www.ebi.ac.uk/pdbsum/5i9v PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5i9v 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=5i9v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5i9v OCA], [~~http~~://pdbe.org/5i9v PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5i9v RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5i9v PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5i9v ProSAT]</span></td></tr>	+
	</table>		</table>
	== Disease ==		== Disease ==
-	[~~[http~~://www.uniprot.org/uniprot/EPHA2_HUMAN EPHA2_HUMAN]] Genetic variations in EPHA2 are the cause of susceptibility to cataract cortical age-related type 2 (ARCC2) [MIM:[~~http~~://omim.org/entry/613020 613020]]. A developmental punctate opacity common in the cortex and present in most lenses. The cataract is white or cerulean, increases in number with age, but rarely affects vision.<ref>PMID:19573808</ref> <ref>PMID:19649315</ref> Defects in EPHA2 are the cause of cataract posterior polar type 1 (CTPP1) [MIM:[~~http~~://omim.org/entry/116600 116600]]. A subcapsular opacity, usually disk-shaped, located at the back of the lens. It can have a marked effect on visual acuity.<ref>PMID:19573808</ref> <ref>PMID:19005574</ref> <ref>PMID:19306328</ref> <ref>PMID:22570727</ref> Note=Overexpressed in several cancer types and promotes malignancy.<ref>PMID:19573808</ref>	+	[https://www.uniprot.org/uniprot/EPHA2_HUMAN EPHA2_HUMAN] Genetic variations in EPHA2 are the cause of susceptibility to cataract cortical age-related type 2 (ARCC2) [MIM:[https://omim.org/entry/613020 613020]. A developmental punctate opacity common in the cortex and present in most lenses. The cataract is white or cerulean, increases in number with age, but rarely affects vision.<ref>PMID:19573808</ref> <ref>PMID:19649315</ref> Defects in EPHA2 are the cause of cataract posterior polar type 1 (CTPP1) [MIM:[https://omim.org/entry/116600 116600]. A subcapsular opacity, usually disk-shaped, located at the back of the lens. It can have a marked effect on visual acuity.<ref>PMID:19573808</ref> <ref>PMID:19005574</ref> <ref>PMID:19306328</ref> <ref>PMID:22570727</ref> Note=Overexpressed in several cancer types and promotes malignancy.<ref>PMID:19573808</ref>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/EPHA2_HUMAN EPHA2_HUMAN]] Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Activated by the ligand ephrin-A1/EFNA1 regulates migration, integrin-mediated adhesion, proliferation and differentiation of cells. Regulates cell adhesion and differentiation through DSG1/desmoglein-1 and inhibition of the ERK1/ERK2 (MAPK3/MAPK1, respectively) signaling pathway. May also participate in UV radiation-induced apoptosis and have a ligand-independent stimulatory effect on chemotactic cell migration. During development, may function in distinctive aspects of pattern formation and subsequently in development of several fetal tissues. Involved for instance in angiogenesis, in early hindbrain development and epithelial proliferation and branching morphogenesis during mammary gland development. Engaged by the ligand ephrin-A5/EFNA5 may regulate lens fiber cells shape and interactions and be important for lens transparency development and maintenance. With ephrin-A2/EFNA2 may play a role in bone remodeling through regulation of osteoclastogenesis and osteoblastogenesis.<ref>PMID:10655584</ref> <ref>PMID:16236711</ref> <ref>PMID:18339848</ref> <ref>PMID:19573808</ref> <ref>PMID:20679435</ref> <ref>PMID:20861311</ref>	+	[https://www.uniprot.org/uniprot/EPHA2_HUMAN EPHA2_HUMAN] Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Activated by the ligand ephrin-A1/EFNA1 regulates migration, integrin-mediated adhesion, proliferation and differentiation of cells. Regulates cell adhesion and differentiation through DSG1/desmoglein-1 and inhibition of the ERK1/ERK2 (MAPK3/MAPK1, respectively) signaling pathway. May also participate in UV radiation-induced apoptosis and have a ligand-independent stimulatory effect on chemotactic cell migration. During development, may function in distinctive aspects of pattern formation and subsequently in development of several fetal tissues. Involved for instance in angiogenesis, in early hindbrain development and epithelial proliferation and branching morphogenesis during mammary gland development. Engaged by the ligand ephrin-A5/EFNA5 may regulate lens fiber cells shape and interactions and be important for lens transparency development and maintenance. With ephrin-A2/EFNA2 may play a role in bone remodeling through regulation of osteoclastogenesis and osteoblastogenesis.<ref>PMID:10655584</ref> <ref>PMID:16236711</ref> <ref>PMID:18339848</ref> <ref>PMID:19573808</ref> <ref>PMID:20679435</ref> <ref>PMID:20861311</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==
-	*[[Ephrin receptor\|Ephrin receptor]]	+	*[[Ephrin receptor 3D structures\|Ephrin receptor 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	~~[[Category: Receptor protein-tyrosine kinase]]~~	+	[[Category: Gande SL]]
-	[[Category: Gande~~, S L~~]]	+	[[Category: Heinzlmeir S]]
-	[[Category: Heinzlmeir, S]]	+	[[Category: Kudlinzki D]]
-	[[Category: Kudlinzki, D]]	+	[[Category: Kuester B]]
-	[[Category: Kuester, B]]	+	[[Category: Linhard VL]]
-	[[Category: Linhard~~, V L~~]]	+	[[Category: Medard G]]
-	[[Category: Medard, G]]	+	[[Category: Saxena K]]
-	[[Category: Saxena, K]]	+	[[Category: Schwalbe H]]
-	[[Category: Schwalbe, H]]	+	[[Category: Sreeramulu S]]
-	[[Category: Sreeramulu, S]]	+
-	~~[[Category: Atp-binding]]~~	+
-	~~[[Category: Receptor]]~~	+
-	~~[[Category: Transferase]]~~	+
-	~~[[Category: Tyrosine-protein kinase~~]]	+

OCA at 05:56, 12 June 2019

2019-06-12T05:56:43Z

←Older revision		Revision as of 05:56, 12 June 2019
Line 32:		Line 32:
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]
-	[[Category: ~~GANDE~~, S L]]	+	[[Category: Gande, S L]]
-	[[Category: ~~HEINZLMEIR~~, S]]	+	[[Category: Heinzlmeir, S]]
-	[[Category: ~~KUDLINZKI~~, D]]	+	[[Category: Kudlinzki, D]]
-	[[Category: ~~KUESTER~~, B]]	+	[[Category: Kuester, B]]
-	[[Category: ~~LINHARD~~, V L]]	+	[[Category: Linhard, V L]]
-	[[Category: ~~MEDARD~~, G]]	+	[[Category: Medard, G]]
-	[[Category: ~~SAXENA~~, K]]	+	[[Category: Saxena, K]]
-	[[Category: ~~SCHWALBE~~, H]]	+	[[Category: Schwalbe, H]]
-	[[Category: ~~SREERAMULU~~, S]]	+	[[Category: Sreeramulu, S]]
	[[Category: Atp-binding]]		[[Category: Atp-binding]]
	[[Category: Receptor]]		[[Category: Receptor]]
	[[Category: Transferase]]		[[Category: Transferase]]
	[[Category: Tyrosine-protein kinase]]		[[Category: Tyrosine-protein kinase]]

OCA at 07:56, 3 April 2019

2019-04-03T07:56:32Z

←Older revision		Revision as of 07:56, 3 April 2019
Line 1:		Line 1:

	==Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with AGS==		==Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with AGS==
-	<StructureSection load='5i9v' size='340' side='right' caption='[[5i9v]], [[Resolution\|resolution]] 1.46Å' scene=''>	+	<StructureSection load='5i9v' size='340' side='right'caption='[[5i9v]], [[Resolution\|resolution]] 1.46Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[5i9v]] 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=5I9V OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5I9V FirstGlance]. <br>		<table><tr><td colspan='2'>[[5i9v]] 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=5I9V OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5I9V FirstGlance]. <br>
Line 30:		Line 30:
	</StructureSection>		</StructureSection>
	[[Category: Human]]		[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]
	[[Category: GANDE, S L]]		[[Category: GANDE, S L]]

OCA at 06:06, 8 March 2018

2018-03-08T06:06:00Z

←Older revision		Revision as of 06:06, 8 March 2018
Line 3:		Line 3:
	<StructureSection load='5i9v' size='340' side='right' caption='[[5i9v]], [[Resolution\|resolution]] 1.46Å' scene=''>		<StructureSection load='5i9v' size='340' side='right' caption='[[5i9v]], [[Resolution\|resolution]] 1.46Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5i9v]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5I9V OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5I9V FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5i9v]] 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=5I9V OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5I9V FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=AGS:PHOSPHOTHIOPHOSPHORIC+ACID-ADENYLATE+ESTER'>AGS</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=AGS:PHOSPHOTHIOPHOSPHORIC+ACID-ADENYLATE+ESTER'>AGS</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">EPHA2, ECK ([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=5i9v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5i9v OCA], [http://pdbe.org/5i9v PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5i9v RCSB], [http://www.ebi.ac.uk/pdbsum/5i9v PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5i9v 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=5i9v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5i9v OCA], [http://pdbe.org/5i9v PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5i9v RCSB], [http://www.ebi.ac.uk/pdbsum/5i9v PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5i9v ProSAT]</span></td></tr>
Line 21:		Line 22:
	</div>		</div>
	<div class="pdbe-citations 5i9v" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 5i9v" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Ephrin receptor\|Ephrin receptor]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Receptor protein-tyrosine kinase]]		[[Category: Receptor protein-tyrosine kinase]]
	[[Category: GANDE, S L]]		[[Category: GANDE, S L]]

OCA at 19:48, 9 December 2016

2016-12-09T19:48:50Z

←Older revision		Revision as of 19:48, 9 December 2016
Line 1:		Line 1:
-	'''Unreleased structure'''

-	The entry ~~5i9v~~ is ~~ON HOLD~~	+	==Crystal Structure of Ephrin A2 (EphA2) Receptor Protein Kinase with AGS==
		+	<StructureSection load='5i9v' size='340' side='right' caption='[[5i9v]], [[Resolution\|resolution]] 1.46Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[5i9v]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5I9V OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5I9V FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=AGS:PHOSPHOTHIOPHOSPHORIC+ACID-ADENYLATE+ESTER'>AGS</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=5i9v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5i9v OCA], [http://pdbe.org/5i9v PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5i9v RCSB], [http://www.ebi.ac.uk/pdbsum/5i9v PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5i9v ProSAT]</span></td></tr>
		+	</table>
		+	== Disease ==
		+	[[http://www.uniprot.org/uniprot/EPHA2_HUMAN EPHA2_HUMAN]] Genetic variations in EPHA2 are the cause of susceptibility to cataract cortical age-related type 2 (ARCC2) [MIM:[http://omim.org/entry/613020 613020]]. A developmental punctate opacity common in the cortex and present in most lenses. The cataract is white or cerulean, increases in number with age, but rarely affects vision.<ref>PMID:19573808</ref> <ref>PMID:19649315</ref> Defects in EPHA2 are the cause of cataract posterior polar type 1 (CTPP1) [MIM:[http://omim.org/entry/116600 116600]]. A subcapsular opacity, usually disk-shaped, located at the back of the lens. It can have a marked effect on visual acuity.<ref>PMID:19573808</ref> <ref>PMID:19005574</ref> <ref>PMID:19306328</ref> <ref>PMID:22570727</ref> Note=Overexpressed in several cancer types and promotes malignancy.<ref>PMID:19573808</ref>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/EPHA2_HUMAN EPHA2_HUMAN]] Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Activated by the ligand ephrin-A1/EFNA1 regulates migration, integrin-mediated adhesion, proliferation and differentiation of cells. Regulates cell adhesion and differentiation through DSG1/desmoglein-1 and inhibition of the ERK1/ERK2 (MAPK3/MAPK1, respectively) signaling pathway. May also participate in UV radiation-induced apoptosis and have a ligand-independent stimulatory effect on chemotactic cell migration. During development, may function in distinctive aspects of pattern formation and subsequently in development of several fetal tissues. Involved for instance in angiogenesis, in early hindbrain development and epithelial proliferation and branching morphogenesis during mammary gland development. Engaged by the ligand ephrin-A5/EFNA5 may regulate lens fiber cells shape and interactions and be important for lens transparency development and maintenance. With ephrin-A2/EFNA2 may play a role in bone remodeling through regulation of osteoclastogenesis and osteoblastogenesis.<ref>PMID:10655584</ref> <ref>PMID:16236711</ref> <ref>PMID:18339848</ref> <ref>PMID:19573808</ref> <ref>PMID:20679435</ref> <ref>PMID:20861311</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	The receptor tyrosine kinase EPHA2 (Ephrin type-A receptor 2) plays important roles in oncogenesis, metastasis and treatment resistance yet therapeutic targeting, drug discovery or investigation of EPHA2 biology is hampered by the lack of appropriate inhibitors and structural information. Here, we used chemical proteomics to survey 235 clinical kinase inhibitors for their kinase selectivity and identified 24 drugs with sub-micromolar affinities for EPHA2. NMR-based conformational dynamics together with nine new co-crystal structures delineated drug-EPHA2 interactions in full detail. The combination of selectivity profiling, structure determination and kinome wide sequence alignment allowed the development of a classification system in which amino acids in the drug binding site of EPHA2 are categorized into key, scaffold, potency and selectivity residues. This scheme should be generally applicable in kinase drug discovery and we anticipate that the provided information will greatly facilitate the development of selective EPHA2 inhibitors in particular and the repurposing of clinical kinase inhibitors in general.

-	~~Authors~~:	+	Chemical proteomics and structural biology define EPHA2 inhibition by clinical kinase drugs.,Heinzlmeir S, Kudlinzki D, Sreeramulu S, Klaeger S, Gande SL, Linhard V, Wilhelm M, Qiao H, Helm D, Ruprecht B, Saxena K, Medard G, Schwalbe H, Kuster B ACS Chem Biol. 2016 Oct 21. PMID:27768280<ref>PMID:27768280</ref>

-	~~Description~~:	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased Structures~~]]	+	</div>
		+	<div class="pdbe-citations 5i9v" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Receptor protein-tyrosine kinase]]
		+	[[Category: GANDE, S L]]
		+	[[Category: HEINZLMEIR, S]]
		+	[[Category: KUDLINZKI, D]]
		+	[[Category: KUESTER, B]]
		+	[[Category: LINHARD, V L]]
		+	[[Category: MEDARD, G]]
		+	[[Category: SAXENA, K]]
		+	[[Category: SCHWALBE, H]]
		+	[[Category: SREERAMULU, S]]
		+	[[Category: Atp-binding]]
		+	[[Category: Receptor]]
		+	[[Category: Transferase]]
		+	[[Category: Tyrosine-protein kinase]]

OCA at 14:16, 15 May 2016

2016-05-15T14:16:03Z

←Older revision		Revision as of 14:16, 15 May 2016
Line 3:		Line 3:
	The entry 5i9v is ON HOLD		The entry 5i9v is ON HOLD

-	Authors: ~~KUDLINZKI, D., LINHARD, V.L., GANDE, S.L., SREERAMULU, S., SAXENA, K., HEINZLMEIR, S., MEDARD, G., KUESTER, B., SCHWALBE, H.~~	+	Authors:

	Description:		Description:
	[[Category: Unreleased Structures]]		[[Category: Unreleased Structures]]
-	[[Category: Kudlinzki, D]]
-	[[Category: Saxena, K]]
-	[[Category: Medard, G]]
-	[[Category: Heinzlmeir, S]]
-	[[Category: Kuester, B]]
-	[[Category: Linhard, V.L]]
-	[[Category: Gande, S.L]]
-	[[Category: Schwalbe, H]]
-	[[Category: Sreeramulu, S]]

OCA: Protected "5i9v" [edit=sysop:move=sysop]

2016-03-02T13:36:38Z

Protected "5i9v" [edit=sysop:move=sysop]

←Older revision

Revision as of 13:36, 2 March 2016

OCA: New page: '''Unreleased structure''' The entry 5i9v is ON HOLD Authors: KUDLINZKI, D., LINHARD, V.L., GANDE, S.L., SREERAMULU, S., SAXENA, K., HEINZLMEIR, S., MEDARD, G., KUESTER, B., SCHWALBE, H...

2016-03-02T13:36:36Z

New page: '''Unreleased structure''' The entry 5i9v is ON HOLD Authors: KUDLINZKI, D., LINHARD, V.L., GANDE, S.L., SREERAMULU, S., SAXENA, K., HEINZLMEIR, S., MEDARD, G., KUESTER, B., SCHWALBE, H...

New page

'''Unreleased structure'''

The entry 5i9v is ON HOLD

Authors: KUDLINZKI, D., LINHARD, V.L., GANDE, S.L., SREERAMULU, S., SAXENA, K., HEINZLMEIR, S., MEDARD, G., KUESTER, B., SCHWALBE, H.

Description:
[[Category: Unreleased Structures]]
[[Category: Kudlinzki, D]]
[[Category: Saxena, K]]
[[Category: Medard, G]]
[[Category: Heinzlmeir, S]]
[[Category: Kuester, B]]
[[Category: Linhard, V.L]]
[[Category: Gande, S.L]]
[[Category: Schwalbe, H]]
[[Category: Sreeramulu, S]]