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{{STRUCTURE_4l7j|  PDB=4l7j  |  SCENE=  }}
===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)===


==Function==
==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)==
[[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>
<StructureSection load='4l7j' size='340' side='right'caption='[[4l7j]], [[Resolution|resolution]] 1.65&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[4l7j]] 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=4L7J OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4L7J FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.651&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1W2:2-[(3AS,7AR)-2-AMINO-3A-(2,4-DIFLUOROPHENYL)-3A,6,7,7A-TETRAHYDRO[1,3]OXAZOLO[4,5-C]PYRIDIN-5(4H)-YL]PYRIDINE-3-CARBONITRILE'>1W2</scene>, <scene name='pdbligand=ACT:ACETATE+ION'>ACT</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=4l7j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4l7j OCA], [https://pdbe.org/4l7j PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4l7j RCSB], [https://www.ebi.ac.uk/pdbsum/4l7j PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4l7j ProSAT]</span></td></tr>
</table>
== 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>  


==About this Structure==
==See Also==
[[4l7j]] is a 1 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=4L7J OCA].
*[[Beta secretase 3D structures|Beta secretase 3D structures]]
 
== References ==
==Reference==
<references/>
<references group="xtra"/><references/>
__TOC__
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Memapsin 2]]
[[Category: Large Structures]]
[[Category: Do, M K.Geck.]]
[[Category: Dutcher D]]
[[Category: Dutcher, D.]]
[[Category: Geck Do MK]]
[[Category: Huestis, M P.]]
[[Category: Huestis MP]]
[[Category: Hunt, K W.]]
[[Category: Hunt KW]]
[[Category: Liu, W.]]
[[Category: Liu W]]
[[Category: Purkey, H E.]]
[[Category: Purkey HE]]
[[Category: Siu, M.]]
[[Category: Siu M]]
[[Category: Smith, D.]]
[[Category: Smith D]]
[[Category: Vigers, G.]]
[[Category: Vigers G]]
[[Category: Volgraf, M.]]
[[Category: Volgraf M]]
[[Category: Wang, W.]]
[[Category: Wang W]]
[[Category: Wu, P.]]
[[Category: Wu P]]
[[Category: Yu, C.]]
[[Category: Yu C]]
[[Category: Aspartic protease]]
[[Category: Hydrolase-hydrolase inhibitor complex]]

Latest revision as of 16:14, 20 September 2023

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)

4l7j, resolution 1.65Å

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