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4l7h
From Proteopedia
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==Diethylaminosulfur Trifluoride-Mediated Intramolecular Cyclization of 2-hydroxy-benzylureas to Fused Bicyclic Aminooxazoline Compounds and Evaluation of Their Biochemical Activity Against Beta-Secretase-1 (BACE-1)== | ==Diethylaminosulfur Trifluoride-Mediated Intramolecular Cyclization of 2-hydroxy-benzylureas to Fused Bicyclic Aminooxazoline Compounds and Evaluation of Their Biochemical Activity Against Beta-Secretase-1 (BACE-1)== | ||
| - | <StructureSection load='4l7h' size='340' side='right' caption='[[4l7h]], [[Resolution|resolution]] 1.85Å' scene=''> | + | <StructureSection load='4l7h' size='340' side='right'caption='[[4l7h]], [[Resolution|resolution]] 1.85Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[4l7h]] is a 1 chain structure with sequence from [ | + | <table><tr><td colspan='2'>[[4l7h]] 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=4L7H OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4L7H FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1W1:2-[(3AR,7AR)-2-AMINO-7A-(2,4-DIFLUOROPHENYL)-3A,6,7,7A-TETRAHYDRO[1,3]OXAZOLO[5,4-C]PYRIDIN-5(4H)-YL]PYRIDINE-3-CARBONITRILE'>1W1</scene>, <scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.85Å</td></tr> |
| - | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1W1:2-[(3AR,7AR)-2-AMINO-7A-(2,4-DIFLUOROPHENYL)-3A,6,7,7A-TETRAHYDRO[1,3]OXAZOLO[5,4-C]PYRIDIN-5(4H)-YL]PYRIDINE-3-CARBONITRILE'>1W1</scene>, <scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</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=4l7h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4l7h OCA], [https://pdbe.org/4l7h PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4l7h RCSB], [https://www.ebi.ac.uk/pdbsum/4l7h PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4l7h ProSAT]</span></td></tr> | |
| - | + | ||
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | |
</table> | </table> | ||
== Function == | == Function == | ||
| - | [ | + | [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> |
==See Also== | ==See Also== | ||
| - | *[[Beta secretase|Beta secretase]] | + | *[[Beta secretase 3D structures|Beta secretase 3D structures]] |
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: | + | [[Category: Homo sapiens]] |
| - | [[Category: | + | [[Category: Large Structures]] |
| - | [[Category: | + | [[Category: Dutcher D]] |
| - | [[Category: | + | [[Category: Geck Do MK]] |
| - | [[Category: Huestis | + | [[Category: Huestis MP]] |
| - | [[Category: Hunt | + | [[Category: Hunt KW]] |
| - | [[Category: Liu | + | [[Category: Liu W]] |
| - | [[Category: Purkey | + | [[Category: Purkey HE]] |
| - | [[Category: Siu | + | [[Category: Siu M]] |
| - | [[Category: Smith | + | [[Category: Smith D]] |
| - | [[Category: Vigers | + | [[Category: Vigers G]] |
| - | [[Category: Volgraf | + | [[Category: Volgraf M]] |
| - | [[Category: Wang | + | [[Category: Wang W]] |
| - | [[Category: Wu | + | [[Category: Wu P]] |
| - | [[Category: Yu | + | [[Category: Yu C]] |
| - | + | ||
| - | + | ||
Current revision
Diethylaminosulfur Trifluoride-Mediated Intramolecular Cyclization of 2-hydroxy-benzylureas to Fused Bicyclic Aminooxazoline Compounds and Evaluation of Their Biochemical Activity Against Beta-Secretase-1 (BACE-1)
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Categories: Homo sapiens | Large Structures | Dutcher D | Geck Do MK | Huestis MP | Hunt KW | Liu W | Purkey HE | Siu M | Smith D | Vigers G | Volgraf M | Wang W | Wu P | Yu C
