5lub - Revision history

OCA at 18:49, 18 October 2023

OCA — Wed, 18 Oct 2023 18:49:56 GMT

←Older revision		Revision as of 18:49, 18 October 2023
Line 3:		Line 3:
	<StructureSection load='5lub' size='340' side='right'caption='[[5lub]], [[Resolution\|resolution]] 2.10Å' scene=''>		<StructureSection load='5lub' size='340' side='right'caption='[[5lub]], [[Resolution\|resolution]] 2.10Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5lub]] is a 2 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=5LUB OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=5LUB FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5lub]] is a 2 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=5LUB OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5LUB FirstGlance]. <br>
-	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat" id="~~ligandDat~~">~~<scene name='pdbligand=3Y7:7-(MORPHOLIN-4-YL)~~-2,1~~,3-BENZOXADIAZOL-4-AMINE'>3Y7</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</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]] 2.1Å</td></tr>
-	<tr id='~~NonStdRes~~'><td class="sblockLbl"><b>[[~~Non-Standard_Residue~~\|~~NonStd Res~~:]]</b></td><td class="sblockDat"><scene name='pdbligand=~~SNN~~:L-3-~~AMINOSUCCINIMIDE~~'>~~SNN~~</scene><~~/td></tr>~~	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=3Y7:7-(MORPHOLIN-4-YL)-2,1,3-BENZOXADIAZOL-4-AMINE'>3Y7</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=SNN:L-3-AMINOSUCCINIMIDE'>SNN</scene></td></tr>
-	~~<tr id~~='~~gene'><td class~~=~~"sblockLbl"><b>[[Gene\|Gene~~:~~]]</b~~></td>~~<td class="sblockDat">LGMN~~, ~~PRSC1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])~~<~~/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=5lub FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5lub OCA], [https://pdbe.org/5lub PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5lub RCSB], [https://www.ebi.ac.uk/pdbsum/5lub PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5lub ProSAT]</span></td></tr>
-	~~<tr id~~='~~activity'><td class~~=~~"sblockLbl"><b>Activity~~:~~</b></td><td class="sblockDat"><span class='plainlinks~~'>~~[http://en.wikipedia.org/wiki/Legumain Legumain], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.34 3.4.22.34]~~ </~~span~~></td></tr>	+
-	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://proteopedia.org/fgij/fg.htm?mol=5lub FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5lub OCA], [~~http~~://pdbe.org/5lub PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5lub RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5lub PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5lub ProSAT]</span></td></tr>	+
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/LGMN_HUMAN LGMN_HUMAN]] Has a strict specificity for hydrolysis of asparaginyl bonds. Can also cleave aspartyl bonds slowly, especially under acidic conditions. May be involved in the processing of proteins for MHC class II antigen presentation in the lysosomal/endosomal system.	+	[https://www.uniprot.org/uniprot/LGMN_HUMAN LGMN_HUMAN] Has a strict specificity for hydrolysis of asparaginyl bonds. Can also cleave aspartyl bonds slowly, especially under acidic conditions. May be involved in the processing of proteins for MHC class II antigen presentation in the lysosomal/endosomal system.
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 25:		Line 23:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	~~[[Category: Legumain]]~~	+	[[Category: Brandstetter H]]
-	[[Category: Brandstetter, H]]	+	[[Category: Dall E]]
-	[[Category: Dall, E]]	+	[[Category: Ye K]]
-	[[Category: Ye, K]]	+
-	~~[[Category: Allosteric inhibitor]]~~	+
-	~~[[Category: Alzheimer's disease]]~~	+
-	~~[[Category: Asparaginyl endopeptidase]]~~	+
-	~~[[Category: Cysteine protease]]~~	+
-	~~[[Category: Hydrolase~~]]	+

OCA at 10:50, 12 August 2020

OCA — Wed, 12 Aug 2020 10:50:39 GMT

←Older revision		Revision as of 10:50, 12 August 2020
Line 1:		Line 1:

	==Crystal structure of human legumain (AEP) in complex with compound 11==		==Crystal structure of human legumain (AEP) in complex with compound 11==
-	<StructureSection load='5lub' size='340' side='right' caption='[[5lub]], [[Resolution\|resolution]] 2.10Å' scene=''>	+	<StructureSection load='5lub' size='340' side='right'caption='[[5lub]], [[Resolution\|resolution]] 2.10Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5lub]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5LUB OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5LUB FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5lub]] is a 2 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=5LUB OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5LUB FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3Y7:7-(MORPHOLIN-4-YL)-2,1,3-BENZOXADIAZOL-4-AMINE'>3Y7</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=3Y7:7-(MORPHOLIN-4-YL)-2,1,3-BENZOXADIAZOL-4-AMINE'>3Y7</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene></td></tr>
	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=SNN:L-3-AMINOSUCCINIMIDE'>SNN</scene></td></tr>		<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=SNN:L-3-AMINOSUCCINIMIDE'>SNN</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">LGMN, PRSC1 ([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/Legumain Legumain], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.34 3.4.22.34] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Legumain Legumain], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.34 3.4.22.34] </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=5lub FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5lub OCA], [http://pdbe.org/5lub PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5lub RCSB], [http://www.ebi.ac.uk/pdbsum/5lub PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5lub ProSAT]</span></td></tr>	+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=5lub FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5lub OCA], [http://pdbe.org/5lub PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5lub RCSB], [http://www.ebi.ac.uk/pdbsum/5lub PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5lub ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 24:		Line 25:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Legumain]]		[[Category: Legumain]]
	[[Category: Brandstetter, H]]		[[Category: Brandstetter, H]]

OCA at 06:58, 5 April 2017

OCA — Wed, 05 Apr 2017 06:58:51 GMT

←Older revision		Revision as of 06:58, 5 April 2017
Line 11:		Line 11:
	== Function ==		== Function ==
	[[http://www.uniprot.org/uniprot/LGMN_HUMAN LGMN_HUMAN]] Has a strict specificity for hydrolysis of asparaginyl bonds. Can also cleave aspartyl bonds slowly, especially under acidic conditions. May be involved in the processing of proteins for MHC class II antigen presentation in the lysosomal/endosomal system.		[[http://www.uniprot.org/uniprot/LGMN_HUMAN LGMN_HUMAN]] Has a strict specificity for hydrolysis of asparaginyl bonds. Can also cleave aspartyl bonds slowly, especially under acidic conditions. May be involved in the processing of proteins for MHC class II antigen presentation in the lysosomal/endosomal system.
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	delta-secretase, also known as asparagine endopeptidase (AEP) or legumain, is a lysosomal cysteine protease that cleaves both amyloid precursor protein (APP) and tau, mediating the amyloid-beta and tau pathology in Alzheimer's disease (AD). Here we report the therapeutic effect of an orally bioactive and brain permeable delta-secretase inhibitor in mouse models of AD. We performed a high-throughput screen and identified a non-toxic and selective delta-secretase inhibitor, termed compound 11, that specifically blocks delta-secretase but not other related cysteine proteases. Co-crystal structure analysis revealed a dual active site-directed and allosteric inhibition mode of this compound class. Chronic treatment of tau P301S and 5XFAD transgenic mice with this inhibitor reduces tau and APP cleavage, ameliorates synapse loss and augments long-term potentiation, resulting in protection of memory. Therefore, these findings demonstrate that this delta-secretase inhibitor may be an effective clinical therapeutic agent towards AD.
		+
		+	Inhibition of delta-secretase improves cognitive functions in mouse models of Alzheimer's disease.,Zhang Z, Obianyo O, Dall E, Du Y, Fu H, Liu X, Kang SS, Song M, Yu SP, Cabrele C, Schubert M, Li X, Wang JZ, Brandstetter H, Ye K Nat Commun. 2017 Mar 27;8:14740. doi: 10.1038/ncomms14740. PMID:28345579<ref>PMID:28345579</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 5lub" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>

OCA at 13:46, 29 March 2017

OCA — Wed, 29 Mar 2017 13:46:55 GMT

←Older revision		Revision as of 13:46, 29 March 2017
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 5lub is ~~ON HOLD until Paper Publication~~	+	==Crystal structure of human legumain (AEP) in complex with compound 11==
-		+	<StructureSection load='5lub' size='340' side='right' caption='[[5lub]], [[Resolution\|resolution]] 2.10Å' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[5lub]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5LUB OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5LUB FirstGlance]. <br>
-	~~Description~~:	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3Y7:7-(MORPHOLIN-4-YL)-2,1,3-BENZOXADIAZOL-4-AMINE'>3Y7</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene></td></tr>
-	[[Category: ~~Unreleased Structures~~]]	+	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=SNN:L-3-AMINOSUCCINIMIDE'>SNN</scene></td></tr>
		+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Legumain Legumain], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.34 3.4.22.34] </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=5lub FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5lub OCA], [http://pdbe.org/5lub PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5lub RCSB], [http://www.ebi.ac.uk/pdbsum/5lub PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5lub ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/LGMN_HUMAN LGMN_HUMAN]] Has a strict specificity for hydrolysis of asparaginyl bonds. Can also cleave aspartyl bonds slowly, especially under acidic conditions. May be involved in the processing of proteins for MHC class II antigen presentation in the lysosomal/endosomal system.
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Legumain]]
		+	[[Category: Brandstetter, H]]
		+	[[Category: Dall, E]]
		+	[[Category: Ye, K]]
		+	[[Category: Allosteric inhibitor]]
		+	[[Category: Alzheimer's disease]]
		+	[[Category: Asparaginyl endopeptidase]]
		+	[[Category: Cysteine protease]]
		+	[[Category: Hydrolase]]

OCA at 16:07, 9 December 2016

OCA — Fri, 09 Dec 2016 16:07:47 GMT

←Older revision		Revision as of 16:07, 9 December 2016
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 5lub is ON HOLD	+	The entry 5lub is ON HOLD until Paper Publication

	Authors:		Authors:

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

OCA — Wed, 14 Sep 2016 13:42:33 GMT

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

←Older revision

Revision as of 13:42, 14 September 2016

OCA: New page: '''Unreleased structure''' The entry 5lub is ON HOLD Authors: Description: Category: Unreleased Structures

OCA — Wed, 14 Sep 2016 13:42:31 GMT

New page: '''Unreleased structure''' The entry 5lub is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 5lub is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]