4yll - Revision history

OCA at 08:02, 27 September 2023

2023-09-27T08:02:08Z

← Older revision		Revision as of 08:02, 27 September 2023
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	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4yll]] 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=4YLL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4YLL FirstGlance]. <br>		<table><tr><td colspan='2'>[[4yll]] 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=4YLL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4YLL FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=4E3:10-BROMO-2-IODO-11H-INDOLO[3,2-C]QUINOLINE-6-CARBOXYLIC+ACID'>4E3</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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]] 1.4Å</td></tr>
			<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=4E3:10-BROMO-2-IODO-11H-INDOLO[3,2-C]QUINOLINE-6-CARBOXYLIC+ACID'>4E3</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</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=4yll FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yll OCA], [https://pdbe.org/4yll PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4yll RCSB], [https://www.ebi.ac.uk/pdbsum/4yll PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4yll ProSAT]</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=4yll FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yll OCA], [https://pdbe.org/4yll PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4yll RCSB], [https://www.ebi.ac.uk/pdbsum/4yll PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4yll ProSAT]</span></td></tr>
	</table>		</table>

OCA at 08:17, 3 May 2023

2023-05-03T08:17:58Z

← Older revision		Revision as of 08:17, 3 May 2023
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	==Crystal structure of DYRK1AA in complex with 10-Bromo-substituted 11H-indolo[3,2-c]quinolone-6-carboxylic acid inhibitor 5t==		==Crystal structure of DYRK1AA in complex with 10-Bromo-substituted 11H-indolo[3,2-c]quinolone-6-carboxylic acid inhibitor 5t==
	<StructureSection load='4yll' size='340' side='right' caption='[[4yll]], [[Resolution\|resolution]] 1.40Å' scene=''>		<StructureSection load='4yll' size='340' side='right'caption='[[4yll]], [[Resolution\|resolution]] 1.40Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4yll]] 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=4YLL OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4YLL FirstGlance]. <br>		<table><tr><td colspan='2'>[[4yll]] 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=4YLL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4YLL FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=4E3:10-BROMO-2-IODO-11H-INDOLO[3,2-C]QUINOLINE-6-CARBOXYLIC+ACID'>4E3</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, ~~<scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>~~		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=4E3:10-BROMO-2-IODO-11H-INDOLO[3,2-C]QUINOLINE-6-CARBOXYLIC+ACID'>4E3</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
	~~<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat">~~<scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</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=4yll FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yll OCA], [https://pdbe.org/4yll PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4yll RCSB], [https://www.ebi.ac.uk/pdbsum/4yll PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4yll ProSAT]</span></td></tr>
	~~<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4ylj\|4ylj]]~~, ~~[[4ylk\|4ylk]]~~<~~/td></tr>~~
	~~<tr id~~='~~gene'><td class~~=~~"sblockLbl"><b>[[Gene\|Gene~~:~~]]</b></td><td class="sblockDat">DYRK1A, DYRK, MNB, MNBH ([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/Dual-specificity_kinase Dual-specificity kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.12.1 2.7.12.1] </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=4yll FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yll OCA], [~~http~~://pdbe.org/4yll PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=4yll RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/4yll PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=4yll ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
	[~~[http~~://www.uniprot.org/uniprot/DYR1A_HUMAN DYR1A_HUMAN]] Defects in DYRK1A are the cause of mental retardation autosomal dominant type 7 (MRD7) [MIM:[~~http~~://omim.org/entry/614104 614104]]. A disease characterized by primary microcephaly, severe mental retardation without speech, anxious autistic behavior, and dysmorphic features, including bitemporal narrowing, deep-set eyes, large simple ears, and a pointed nasal tip. Mental retardation is characterized by significantly below average general intellectual functioning associated with impairments in adaptative behavior and manifested during the developmental period.<ref>PMID:21294719</ref>		[https://www.uniprot.org/uniprot/DYR1A_HUMAN DYR1A_HUMAN] Defects in DYRK1A are the cause of mental retardation autosomal dominant type 7 (MRD7) [MIM:[https://omim.org/entry/614104 614104]. A disease characterized by primary microcephaly, severe mental retardation without speech, anxious autistic behavior, and dysmorphic features, including bitemporal narrowing, deep-set eyes, large simple ears, and a pointed nasal tip. Mental retardation is characterized by significantly below average general intellectual functioning associated with impairments in adaptative behavior and manifested during the developmental period.<ref>PMID:21294719</ref>
	== Function ==		== Function ==
	[~~[http~~://www.uniprot.org/uniprot/DYR1A_HUMAN DYR1A_HUMAN]] May play a role in a signaling pathway regulating nuclear functions of cell proliferation. Phosphorylates serine, threonine and tyrosine residues in its sequence and in exogenous substrates.<ref>PMID:8769099</ref>		[https://www.uniprot.org/uniprot/DYR1A_HUMAN DYR1A_HUMAN] May play a role in a signaling pathway regulating nuclear functions of cell proliferation. Phosphorylates serine, threonine and tyrosine residues in its sequence and in exogenous substrates.<ref>PMID:8769099</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: ~~Dual-specificity kinase~~]]		[[Category: Homo sapiens]]
	[[Category: ~~Human~~]]		[[Category: Large Structures]]
	[[Category: Arrowsmith~~, C H~~]]		[[Category: Arrowsmith CH]]
	[[Category: Bountra, C]]		[[Category: Bountra C]]
	[[Category: Chaikuad, A]]		[[Category: Chaikuad A]]
	~~[[Category: Delft, F von~~]]		[[Category: Edwards AM]]
	[[Category: Edwards~~, A M~~]]		[[Category: Falke H]]
	[[Category: Falke, H]]		[[Category: Knapp S]]
	[[Category: Knapp, S]]		[[Category: Krojer T]]
	[[Category: Krojer, T]]		[[Category: Kunick C]]
	[[Category: Kunick, C]]		[[Category: Von Delft F]]
	[[Category: ~~Structural genomic]]~~
	~~[[Category: Halogen]]~~
	~~[[Category: Inhibitor]]~~
	~~[[Category: Sgc]]~~
	~~[[Category: Transferase-transferase inhibitor complex~~]]

OCA at 09:40, 22 November 2017

2017-11-22T09:40:23Z

← Older revision		Revision as of 09:40, 22 November 2017
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	<StructureSection load='4yll' size='340' side='right' caption='[[4yll]], [[Resolution\|resolution]] 1.40Å' scene=''>		<StructureSection load='4yll' size='340' side='right' caption='[[4yll]], [[Resolution\|resolution]] 1.40Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4yll]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4YLL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4YLL FirstGlance]. <br>		<table><tr><td colspan='2'>[[4yll]] 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=4YLL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4YLL FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=4E3:10-BROMO-2-IODO-11H-INDOLO[3,2-C]QUINOLINE-6-CARBOXYLIC+ACID'>4E3</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=4E3:10-BROMO-2-IODO-11H-INDOLO[3,2-C]QUINOLINE-6-CARBOXYLIC+ACID'>4E3</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene></td></tr>		<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4ylj\|4ylj]], [[4ylk\|4ylk]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4ylj\|4ylj]], [[4ylk\|4ylk]]</td></tr>
			<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">DYRK1A, DYRK, MNB, MNBH ([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/Dual-specificity_kinase Dual-specificity kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.12.1 2.7.12.1] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Dual-specificity_kinase Dual-specificity kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.12.1 2.7.12.1] </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=4yll FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yll OCA], [http://pdbe.org/4yll PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4yll RCSB], [http://www.ebi.ac.uk/pdbsum/4yll PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4yll 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=4yll FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yll OCA], [http://pdbe.org/4yll PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4yll RCSB], [http://www.ebi.ac.uk/pdbsum/4yll PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4yll ProSAT]</span></td></tr>
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	</StructureSection>		</StructureSection>
	[[Category: Dual-specificity kinase]]		[[Category: Dual-specificity kinase]]
			[[Category: Human]]
	[[Category: Arrowsmith, C H]]		[[Category: Arrowsmith, C H]]
	[[Category: Bountra, C]]		[[Category: Bountra, C]]

OCA at 09:59, 10 March 2017

2017-03-10T09:59:35Z

← Older revision		Revision as of 09:59, 10 March 2017
Line 1:		Line 1:

	==Crystal structure of DYRK1AA in complex with 10-Bromo-substituted 11H-indolo[3,2-c]quinolone-6-carboxylic acid inhibitor 5t==		==Crystal structure of DYRK1AA in complex with 10-Bromo-substituted 11H-indolo[3,2-c]quinolone-6-carboxylic acid inhibitor 5t==
	<StructureSection load='4yll' size='340' side='right' caption='[[4yll]], [[Resolution\|resolution]] 1.40Å' scene=''>		<StructureSection load='4yll' size='340' side='right' caption='[[4yll]], [[Resolution\|resolution]] 1.40Å' scene=''>
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	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4ylj\|4ylj]], [[4ylk\|4ylk]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4ylj\|4ylj]], [[4ylk\|4ylk]]</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Dual-specificity_kinase Dual-specificity kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.12.1 2.7.12.1] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Dual-specificity_kinase Dual-specificity kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.12.1 2.7.12.1] </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=4yll FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yll OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4yll RCSB], [http://www.ebi.ac.uk/pdbsum/4yll PDBsum]</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=4yll FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yll OCA], [http://pdbe.org/4yll PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4yll RCSB], [http://www.ebi.ac.uk/pdbsum/4yll PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4yll ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
Line 21:		Line 22:
	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	</div>		</div>
			<div class="pdbe-citations 4yll" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>

OCA at 13:57, 26 March 2015

2015-03-26T13:57:09Z

← Older revision		Revision as of 13:57, 26 March 2015
Line 1:		Line 1:
	'''~~Unreleased~~ structure'''		==Crystal structure of DYRK1AA in complex with 10-Bromo-substituted 11H-indolo[3,2-c]quinolone-6-carboxylic acid inhibitor 5t==
			<StructureSection load='4yll' size='340' side='right' caption='[[4yll]], [[Resolution\|resolution]] 1.40Å' scene=''>
			== Structural highlights ==
			<table><tr><td colspan='2'>[[4yll]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4YLL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4YLL FirstGlance]. <br>
			</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=4E3:10-BROMO-2-IODO-11H-INDOLO[3,2-C]QUINOLINE-6-CARBOXYLIC+ACID'>4E3</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
			<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene></td></tr>
			<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4ylj\|4ylj]], [[4ylk\|4ylk]]</td></tr>
			<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Dual-specificity_kinase Dual-specificity kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.12.1 2.7.12.1] </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=4yll FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4yll OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4yll RCSB], [http://www.ebi.ac.uk/pdbsum/4yll PDBsum]</span></td></tr>
			</table>
			== Disease ==
			[[http://www.uniprot.org/uniprot/DYR1A_HUMAN DYR1A_HUMAN]] Defects in DYRK1A are the cause of mental retardation autosomal dominant type 7 (MRD7) [MIM:[http://omim.org/entry/614104 614104]]. A disease characterized by primary microcephaly, severe mental retardation without speech, anxious autistic behavior, and dysmorphic features, including bitemporal narrowing, deep-set eyes, large simple ears, and a pointed nasal tip. Mental retardation is characterized by significantly below average general intellectual functioning associated with impairments in adaptative behavior and manifested during the developmental period.<ref>PMID:21294719</ref>
			== Function ==
			[[http://www.uniprot.org/uniprot/DYR1A_HUMAN DYR1A_HUMAN]] May play a role in a signaling pathway regulating nuclear functions of cell proliferation. Phosphorylates serine, threonine and tyrosine residues in its sequence and in exogenous substrates.<ref>PMID:8769099</ref>
			<div style="background-color:#fffaf0;">
			== Publication Abstract from PubMed ==
			The protein kinase DYRK1A has been suggested to act as one of the intracellular regulators contributing to neurological alterations found in individuals with Down syndrome. For an assessment of the role of DYRK1A, selective synthetic inhibitors are valuable pharmacological tools. However, the DYRK1A inhibitors described in the literature so far either are not sufficiently selective or have not been tested against closely related kinases from the DYRK and the CLK protein kinase families. The aim of this study was the identification of DYRK1A inhibitors exhibiting selectivity versus the structurally and functionally closely related DYRK and CLK isoforms. Structure modification of the screening hit 11H-indolo[3,2-c]quinoline-6-carboxylic acid revealed structure-activity relationships for kinase inhibition and enabled the design of 10-iodo-substituted derivatives as very potent DYRK1A inhibitors with considerable selectivity against CLKs. X-ray structure determination of three 11H-indolo[3,2-c]quinoline-6-carboxylic acids cocrystallized with DYRK1A confirmed the predicted binding mode within the ATP binding site.

	~~The entry 4yll is ON HOLD~~		10-Iodo-11H-indolo[3,2-c]quinoline-6-carboxylic Acids Are Selective Inhibitors of DYRK1A.,Falke H, Chaikuad A, Becker A, Loaec N, Lozach O, Abu Jhaisha S, Becker W, Jones PG, Preu L, Baumann K, Knapp S, Meijer L, Kunick C J Med Chem. 2015 Mar 23. PMID:25730262<ref>PMID:25730262</ref>

	~~Authors: Chaikuad~~, A.~~, Falke, H~~.~~, Krojer, T~~.~~, von Delft, F., Arrowsmith, C.H., Edwards, A.M., Bountra, C., Kunick, C., Knapp, S., Structural Genomics Consortium (SGC)~~		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
			</div>
	~~Description~~: ~~Crystal structure of DYRK1AA in complex with 10~~-~~Bromo-substituted 11H-indolo~~[3,~~2-c~~]~~quinolone-6-carboxylic acid inhibitor 5t~~		== References ==
	[[Category: ~~Unreleased Structures~~]]		<references/>
			__TOC__
			</StructureSection>
			[[Category: Dual-specificity kinase]]
			[[Category: Arrowsmith, C H]]
			[[Category: Bountra, C]]
	[[Category: Chaikuad, A]]		[[Category: Chaikuad, A]]
	[[Category: ~~Kunick~~, C]]		[[Category: Delft, F von]]
			[[Category: Edwards, A M]]
	[[Category: Falke, H]]		[[Category: Falke, H]]
	[[Category: Knapp, S]]		[[Category: Knapp, S]]
	[[Category: Krojer, T]]		[[Category: Krojer, T]]
	[[Category: ~~Bountra~~, C]]		[[Category: Kunick, C]]
	[[Category: ~~Arrowsmith, C.H~~]]		[[Category: Structural genomic]]
	[[Category: ~~Von Delft, F~~]]		[[Category: Halogen]]
	[[Category: ~~Edwards, A.M~~]]		[[Category: Inhibitor]]
	[[Category: ~~Structural Genomics Consortium (~~Sgc)]]		[[Category: Sgc]]
			[[Category: Transferase-transferase inhibitor complex]]

OCA: Protected "4yll" [edit=sysop:move=sysop]

2015-03-11T10:48:27Z

Protected "4yll" [edit=sysop:move=sysop]

← Older revision	Revision as of 10:48, 11 March 2015
(No difference)

OCA: New page: '''Unreleased structure''' The entry 4yll is ON HOLD Authors: Chaikuad, A., Falke, H., Krojer, T., von Delft, F., Arrowsmith, C.H., Edwards, A.M., Bountra, C., Kunick, C., Knapp, S., St...

2015-03-11T10:48:25Z

New page: '''Unreleased structure''' The entry 4yll is ON HOLD Authors: Chaikuad, A., Falke, H., Krojer, T., von Delft, F., Arrowsmith, C.H., Edwards, A.M., Bountra, C., Kunick, C., Knapp, S., St...

New page

'''Unreleased structure'''

The entry 4yll is ON HOLD

Authors: Chaikuad, A., Falke, H., Krojer, T., von Delft, F., Arrowsmith, C.H., Edwards, A.M., Bountra, C., Kunick, C., Knapp, S., Structural Genomics Consortium (SGC)

Description: Crystal structure of DYRK1AA in complex with 10-Bromo-substituted 11H-indolo[3,2-c]quinolone-6-carboxylic acid inhibitor 5t
[[Category: Unreleased Structures]]
[[Category: Chaikuad, A]]
[[Category: Kunick, C]]
[[Category: Falke, H]]
[[Category: Knapp, S]]
[[Category: Krojer, T]]
[[Category: Bountra, C]]
[[Category: Arrowsmith, C.H]]
[[Category: Von Delft, F]]
[[Category: Edwards, A.M]]
[[Category: Structural Genomics Consortium (Sgc)]]