4fse - Revision history

OCA at 20:08, 19 October 2022

OCA — Wed, 19 Oct 2022 20:08:45 GMT

←Older revision		Revision as of 20:08, 19 October 2022
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	<StructureSection load='4fse' size='340' side='right'caption='[[4fse]], [[Resolution\|resolution]] 2.65Å' scene=''>		<StructureSection load='4fse' size='340' side='right'caption='[[4fse]], [[Resolution\|resolution]] 2.65Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4fse]] is a 4 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=4FSE OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4FSE FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4fse]] is a 4 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=4FSE OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4FSE FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0VA:N-[N-(4-AMINO-3,5-DICHLOROBENZYL)CARBAMIMIDOYL]-3-(4-METHOXYPHENYL)-5-METHYL-1,2-THIAZOLE-4-CARBOXAMIDE'>0VA</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</scene~~></td></tr>~~	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0VA:N-[N-(4-AMINO-3,5-DICHLOROBENZYL)CARBAMIMIDOYL]-3-(4-METHOXYPHENYL)-5-METHYL-1,2-THIAZOLE-4-CARBOXAMIDE'>0VA</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</scene></td></tr>
-	~~<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4fsl\|4fsl]]</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=4fse FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4fse OCA], [https://pdbe.org/4fse PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4fse RCSB], [https://www.ebi.ac.uk/pdbsum/4fse PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4fse ProSAT]</span></td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">BACE1, BACE, KIAA1149 ([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/Memapsin_2 Memapsin 2], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.46 3.4.23.46] </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=4fse FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4fse OCA], [~~http~~://pdbe.org/4fse PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=4fse RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/4fse PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=4fse ProSAT]</span></td></tr>	+
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/BACE1_HUMAN BACE1_HUMAN]] Responsible for the proteolytic processing of the amyloid precursor protein (APP). Cleaves at the N-terminus of the A-beta peptide sequence, between residues 671 and 672 of APP, leads to the generation and extracellular release of beta-cleaved soluble APP, and a corresponding cell-associated C-terminal fragment which is later released by gamma-secretase.<ref>PMID:10677483</ref> <ref>PMID:20354142</ref>	+	[https://www.uniprot.org/uniprot/BACE1_HUMAN BACE1_HUMAN] Responsible for the proteolytic processing of the amyloid precursor protein (APP). Cleaves at the N-terminus of the A-beta peptide sequence, between residues 671 and 672 of APP, leads to the generation and extracellular release of beta-cleaved soluble APP, and a corresponding cell-associated C-terminal fragment which is later released by gamma-secretase.<ref>PMID:10677483</ref> <ref>PMID:20354142</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 28:		Line 25:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	~~[[Category: Memapsin 2]]~~	+	[[Category: Muckelbauer JK]]
-	[[Category: Muckelbauer~~, J K]]~~	+
-	~~[[Category: Alzheimer's disease]]~~	+
-	~~[[Category: Aspartic protease]]~~	+
-	~~[[Category: Base]]~~	+
-	~~[[Category: Beta-secretase]]~~	+
-	~~[[Category: Hydrolase-inhibitor complex~~]]	+

OCA at 11:53, 17 July 2019

OCA — Wed, 17 Jul 2019 11:53:21 GMT

←Older revision		Revision as of 11:53, 17 July 2019
Line 1:		Line 1:

	==crystal structure of beta-site app-cleaving enzyme 1 (bace-wt) complex with N-(N-(4-amino-3,5- dichlorobenzyl)carbamimidoyl)-3-(4-methoxyphenyl)-5- methyl-4-isothiazolecarboxamide==		==crystal structure of beta-site app-cleaving enzyme 1 (bace-wt) complex with N-(N-(4-amino-3,5- dichlorobenzyl)carbamimidoyl)-3-(4-methoxyphenyl)-5- methyl-4-isothiazolecarboxamide==
-	<StructureSection load='4fse' size='340' side='right' caption='[[4fse]], [[Resolution\|resolution]] 2.65Å' scene=''>	+	<StructureSection load='4fse' size='340' side='right'caption='[[4fse]], [[Resolution\|resolution]] 2.65Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4fse]] is a 4 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=4FSE OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4FSE FirstGlance]. <br>		<table><tr><td colspan='2'>[[4fse]] is a 4 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=4FSE OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4FSE FirstGlance]. <br>
Line 23:		Line 23:

	==See Also==		==See Also==
-	*[[Beta secretase\|Beta secretase]]	+	*[[Beta secretase 3D structures\|Beta secretase 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
Line 29:		Line 29:
	</StructureSection>		</StructureSection>
	[[Category: Human]]		[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Memapsin 2]]		[[Category: Memapsin 2]]
	[[Category: Muckelbauer, J K]]		[[Category: Muckelbauer, J K]]

OCA at 16:51, 5 August 2016

OCA — Fri, 05 Aug 2016 16:51:32 GMT

←Older revision		Revision as of 16:51, 5 August 2016
Line 1:		Line 1:
		+
	==crystal structure of beta-site app-cleaving enzyme 1 (bace-wt) complex with N-(N-(4-amino-3,5- dichlorobenzyl)carbamimidoyl)-3-(4-methoxyphenyl)-5- methyl-4-isothiazolecarboxamide==		==crystal structure of beta-site app-cleaving enzyme 1 (bace-wt) complex with N-(N-(4-amino-3,5- dichlorobenzyl)carbamimidoyl)-3-(4-methoxyphenyl)-5- methyl-4-isothiazolecarboxamide==
	<StructureSection load='4fse' size='340' side='right' caption='[[4fse]], [[Resolution\|resolution]] 2.65Å' scene=''>		<StructureSection load='4fse' size='340' side='right' caption='[[4fse]], [[Resolution\|resolution]] 2.65Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4fse]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/~~Homo_sapiens Homo sapiens~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4FSE OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4FSE FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4fse]] is a 4 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=4FSE OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4FSE FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0VA:N-[N-(4-AMINO-3,5-DICHLOROBENZYL)CARBAMIMIDOYL]-3-(4-METHOXYPHENYL)-5-METHYL-1,2-THIAZOLE-4-CARBOXAMIDE'>0VA</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0VA:N-[N-(4-AMINO-3,5-DICHLOROBENZYL)CARBAMIMIDOYL]-3-(4-METHOXYPHENYL)-5-METHYL-1,2-THIAZOLE-4-CARBOXAMIDE'>0VA</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4fsl\|4fsl]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4fsl\|4fsl]]</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">BACE1, BACE, KIAA1149 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 ~~Homo sapiens~~])</td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">BACE1, BACE, KIAA1149 ([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/Memapsin_2 Memapsin 2], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.46 3.4.23.46] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Memapsin_2 Memapsin 2], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.46 3.4.23.46] </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=4fse FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4fse OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4fse RCSB], [http://www.ebi.ac.uk/pdbsum/4fse 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=4fse FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4fse OCA], [http://pdbe.org/4fse PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4fse RCSB], [http://www.ebi.ac.uk/pdbsum/4fse PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4fse ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 19:		Line 20:
	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 4fse" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
Line 26:		Line 28:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Homo sapiens~~]]	+	[[Category: Human]]
	[[Category: Memapsin 2]]		[[Category: Memapsin 2]]
	[[Category: Muckelbauer, J K]]		[[Category: Muckelbauer, J K]]

OCA at 04:10, 25 December 2014

OCA — Thu, 25 Dec 2014 04:10:45 GMT

←Older revision		Revision as of 04:10, 25 December 2014
Line 9:		Line 9:
	<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=4fse FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4fse OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4fse RCSB], [http://www.ebi.ac.uk/pdbsum/4fse 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=4fse FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4fse OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4fse RCSB], [http://www.ebi.ac.uk/pdbsum/4fse PDBsum]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/BACE1_HUMAN BACE1_HUMAN]] Responsible for the proteolytic processing of the amyloid precursor protein (APP). Cleaves at the N-terminus of the A-beta peptide sequence, between residues 671 and 672 of APP, leads to the generation and extracellular release of beta-cleaved soluble APP, and a corresponding cell-associated C-terminal fragment which is later released by gamma-secretase.<ref>PMID:10677483</ref> <ref>PMID:20354142</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==

OCA at 11:50, 21 December 2014

OCA — Sun, 21 Dec 2014 11:50:03 GMT

←Older revision		Revision as of 11:50, 21 December 2014
Line 1:		Line 1:
-	~~{{STRUCTURE_4fse\| PDB=4fse \| SCENE= }}~~	+	==crystal structure of beta-site app-cleaving enzyme 1 (bace-wt) complex with N-(N-(4-amino-3,5- dichlorobenzyl)carbamimidoyl)-3-(4-methoxyphenyl)-5- methyl-4-isothiazolecarboxamide==
-	===crystal structure of beta-site app-cleaving enzyme 1 (bace-wt) complex with N-(N-(4-amino-3,5- dichlorobenzyl)carbamimidoyl)-3-(4-methoxyphenyl)-5- methyl-4-isothiazolecarboxamide===	+	<StructureSection load='4fse' size='340' side='right' caption='[[4fse]], [[Resolution\|resolution]] 2.65Å' scene=''>
-	~~{{ABSTRACT_PUBMED_23030502}}~~	+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[4fse]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4FSE OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4FSE FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0VA:N-[N-(4-AMINO-3,5-DICHLOROBENZYL)CARBAMIMIDOYL]-3-(4-METHOXYPHENYL)-5-METHYL-1,2-THIAZOLE-4-CARBOXAMIDE'>0VA</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</scene></td></tr>
		+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4fsl\|4fsl]]</td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">BACE1, BACE, KIAA1149 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>
		+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Memapsin_2 Memapsin 2], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.23.46 3.4.23.46] </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=4fse FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4fse OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4fse RCSB], [http://www.ebi.ac.uk/pdbsum/4fse PDBsum]</span></td></tr>
		+	</table>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	This report describes the discovery and optimization of a BACE-1 inhibitor series containing an unusual acyl guanidine chemotype that was originally synthesized as part of a 6041-membered solid-phase library. The synthesis of multiple follow-up solid- and solution-phase libraries facilitated the optimization of the original micromolar hit into a single-digit nanomolar BACE-1 inhibitor in both radioligand binding and cell-based functional assay formats. The X-ray structure of representative inhibitors bound to BACE-1 revealed a number of key ligand:protein interactions, including a hydrogen bond between the side chain amide of flap residue Gln73 and the acyl guanidine carbonyl group, and a cation-pi interaction between Arg235 and the isothiazole 4-methoxyphenyl substituent. Following subcutaneous administration in rats, an acyl guanidine inhibitor with single-digit nanomolar activity in cells afforded good plasma exposures and a dose-dependent reduction in plasma Abeta levels, but poor brain exposure was observed (likely due to Pgp-mediated efflux), and significant reductions in brain Abeta levels were not obtained.

-	~~==Function==~~	+	Acyl guanidine inhibitors of beta-secretase (BACE-1): optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis.,Gerritz SW, Zhai W, Shi S, Zhu S, Toyn JH, Meredith JE Jr, Iben LG, Burton CR, Albright CF, Good AC, Tebben AJ, Muckelbauer JK, Camac DM, Metzler W, Cook LS, Padmanabha R, Lentz KA, Sofia MJ, Poss MA, Macor JE, Thompson LA 3rd J Med Chem. 2012 Nov 8;55(21):9208-23. doi: 10.1021/jm300931y. Epub 2012 Oct 2. PMID:23030502<ref>PMID:23030502</ref>
-	~~[[http://www.uniprot.org/uniprot/BACE1_HUMAN BACE1_HUMAN]] Responsible for the proteolytic processing~~ of ~~the amyloid precursor protein~~ (~~APP). Cleaves at the N~~-~~terminus~~ of ~~the A~~-~~beta peptide sequence, between residues 671~~ and ~~672 of APP, leads to the generation and extracellular release of beta~~-~~cleaved soluble APP~~, ~~and a corresponding cell~~-~~associated C-terminal fragment which is later released by gamma-secretase~~.~~<ref>PMID~~:~~10677483<~~/~~ref>~~ <ref>PMID:~~20354142~~</ref>	+

-	~~==About this Structure==~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	~~[[4fse]] is~~ a ~~4 chain structure with sequence from [http://en~~.~~wikipedia~~.~~org/wiki/Homo_sapiens Homo sapiens]~~. ~~Full crystallographic information is available from [http:~~/~~/oca.weizmann.ac.il/oca-bin/ocashort?id=4FSE OCA].~~	+	</div>

	==See Also==		==See Also==
	*[[Beta secretase\|Beta secretase]]		*[[Beta secretase\|Beta secretase]]
-		+	== References ==
-	==~~Reference~~==	+	<references/>
-	~~<ref group="xtra">PMID:023030502</ref>~~<references ~~group="xtra"~~/><~~references~~/>	+	__TOC__
		+	</StructureSection>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Memapsin 2]]		[[Category: Memapsin 2]]
-	[[Category: Muckelbauer, J K.]]	+	[[Category: Muckelbauer, J K]]
	[[Category: Alzheimer's disease]]		[[Category: Alzheimer's disease]]
	[[Category: Aspartic protease]]		[[Category: Aspartic protease]]
Line 22:		Line 32:
	[[Category: Beta-secretase]]		[[Category: Beta-secretase]]
	[[Category: Hydrolase-inhibitor complex]]		[[Category: Hydrolase-inhibitor complex]]
-	[[Category: Memapsin 2]]

OCA at 14:34, 10 July 2013

OCA — Wed, 10 Jul 2013 14:34:36 GMT

←Older revision		Revision as of 14:34, 10 July 2013
Line 1:		Line 1:
-	[[Image:4fse.jpg\|left\|200px]]
-
	{{STRUCTURE_4fse\| PDB=4fse \| SCENE= }}		{{STRUCTURE_4fse\| PDB=4fse \| SCENE= }}
-
	===crystal structure of beta-site app-cleaving enzyme 1 (bace-wt) complex with N-(N-(4-amino-3,5- dichlorobenzyl)carbamimidoyl)-3-(4-methoxyphenyl)-5- methyl-4-isothiazolecarboxamide===		===crystal structure of beta-site app-cleaving enzyme 1 (bace-wt) complex with N-(N-(4-amino-3,5- dichlorobenzyl)carbamimidoyl)-3-(4-methoxyphenyl)-5- methyl-4-isothiazolecarboxamide===
		+	{{ABSTRACT_PUBMED_23030502}}

		+	==Function==
		+	[[http://www.uniprot.org/uniprot/BACE1_HUMAN BACE1_HUMAN]] Responsible for the proteolytic processing of the amyloid precursor protein (APP). Cleaves at the N-terminus of the A-beta peptide sequence, between residues 671 and 672 of APP, leads to the generation and extracellular release of beta-cleaved soluble APP, and a corresponding cell-associated C-terminal fragment which is later released by gamma-secretase.<ref>PMID:10677483</ref> <ref>PMID:20354142</ref>

	==About this Structure==		==About this Structure==
-	[[4fse]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4FSE OCA].	+	[[4fse]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4FSE OCA].
		+
		+	==See Also==
		+	*[[Beta secretase\|Beta secretase]]
		+
		+	==Reference==
		+	<ref group="xtra">PMID:023030502</ref><references group="xtra"/><references/>
		+	[[Category: Homo sapiens]]
	[[Category: Memapsin 2]]		[[Category: Memapsin 2]]
	[[Category: Muckelbauer, J K.]]		[[Category: Muckelbauer, J K.]]

OCA at 07:28, 10 October 2012

OCA — Wed, 10 Oct 2012 07:28:17 GMT

←Older revision		Revision as of 07:28, 10 October 2012
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-	~~'''Unreleased structure'''~~	+	[[Image:4fse.jpg\|left\|200px]]

-	~~The entry~~ 4fse ~~is ON HOLD~~ ~~until Paper Publication~~	+	{{STRUCTURE_4fse\| PDB=4fse \| SCENE= }}

-	~~Authors: Muckelbauer~~, ~~J.K.~~	+	===crystal structure of beta-site app-cleaving enzyme 1 (bace-wt) complex with N-(N-(4-amino-3,5- dichlorobenzyl)carbamimidoyl)-3-(4-methoxyphenyl)-5- methyl-4-isothiazolecarboxamide===

-	~~Description~~: ~~crystal structure of beta~~-~~site app~~-~~cleaving enzyme 1 (bace~~-~~wt)~~ complex ~~with N-(N-(4-amino-3,5-dichlorobenzyl)carbamimidoyl)-3-(4-methoxyphenyl)-5-methyl-4-isothiazolecarboxamide~~	+
		+	==About this Structure==
		+	[[4fse]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4FSE OCA].
		+	[[Category: Memapsin 2]]
		+	[[Category: Muckelbauer, J K.]]
		+	[[Category: Alzheimer's disease]]
		+	[[Category: Aspartic protease]]
		+	[[Category: Base]]
		+	[[Category: Beta-secretase]]
		+	[[Category: Hydrolase-inhibitor complex]]
		+	[[Category: Memapsin 2]]

OCA at 05:20, 15 August 2012

OCA — Wed, 15 Aug 2012 05:20:08 GMT

←Older revision		Revision as of 05:20, 15 August 2012
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 4fse is ON HOLD	+	The entry 4fse is ON HOLD until Paper Publication

	Authors: Muckelbauer, J.K.		Authors: Muckelbauer, J.K.

	Description: crystal structure of beta-site app-cleaving enzyme 1 (bace-wt) complex with N-(N-(4-amino-3,5-dichlorobenzyl)carbamimidoyl)-3-(4-methoxyphenyl)-5-methyl-4-isothiazolecarboxamide		Description: crystal structure of beta-site app-cleaving enzyme 1 (bace-wt) complex with N-(N-(4-amino-3,5-dichlorobenzyl)carbamimidoyl)-3-(4-methoxyphenyl)-5-methyl-4-isothiazolecarboxamide

OCA at 05:02, 18 July 2012

OCA — Wed, 18 Jul 2012 05:02:58 GMT

←Older revision		Revision as of 05:02, 18 July 2012
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	Authors: Muckelbauer, J.K.		Authors: Muckelbauer, J.K.

-	Description: ~~CRYSTAL STRUCTURE OF BETA~~-~~SITE APP~~-~~CLEAVING ENZYME~~ 1 (~~BACE~~-WT) ~~COMPLEX WITH~~ N-(N-(4-~~AMINO~~-3,5-~~DICHLOROBENZYL~~)~~CARBAMIMIDOYL~~)-3-(4-~~METHOXYPHENYL~~)-5-~~METHYL~~-4-~~ISOTHIAZOLECARBOXAMIDE~~	+	Description: crystal structure of beta-site app-cleaving enzyme 1 (bace-wt) complex with N-(N-(4-amino-3,5-dichlorobenzyl)carbamimidoyl)-3-(4-methoxyphenyl)-5-methyl-4-isothiazolecarboxamide

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

OCA — Wed, 04 Jul 2012 07:21:30 GMT

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

←Older revision

Revision as of 07:21, 4 July 2012