2b8v: Difference between revisions
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<StructureSection load='2b8v' size='340' side='right'caption='[[2b8v]], [[Resolution|resolution]] 1.80Å' scene=''> | <StructureSection load='2b8v' size='340' side='right'caption='[[2b8v]], [[Resolution|resolution]] 1.80Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[2b8v]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/ | <table><tr><td colspan='2'>[[2b8v]] 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=2B8V OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2B8V FirstGlance]. <br> | ||
</td></tr><tr id=' | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.8Å</td></tr> | ||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=3BN:3-BENZOYL-N-[(1S,2R)-1-BENZYL-3-(CYCLOPROPYLAMINO)-2-HYDROXYPROPYL]-5-[METHYL(METHYLSULFONYL)AMINO]BENZAMIDE'>3BN</scene></td></tr> | |||
<tr id=' | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2b8v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2b8v OCA], [https://pdbe.org/2b8v PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2b8v RCSB], [https://www.ebi.ac.uk/pdbsum/2b8v PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2b8v 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=2b8v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2b8v OCA], [https://pdbe.org/2b8v PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2b8v RCSB], [https://www.ebi.ac.uk/pdbsum/2b8v PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2b8v ProSAT]</span></td></tr> | ||
</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> | |||
== Evolutionary Conservation == | == Evolutionary Conservation == | ||
[[Image:Consurf_key_small.gif|200px|right]] | [[Image:Consurf_key_small.gif|200px|right]] | ||
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__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: | [[Category: Homo sapiens]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
[[Category: Coburn CA]] | |||
[[Category: Coburn | [[Category: Crouthamel M-C]] | ||
[[Category: Crouthamel | [[Category: Graham SL]] | ||
[[Category: Graham | [[Category: Holloway MK]] | ||
[[Category: Holloway | [[Category: Lai M-T]] | ||
[[Category: Lai | [[Category: Munshi SK]] | ||
[[Category: Munshi | [[Category: Pietrak BL]] | ||
[[Category: Pietrak | [[Category: Stachel SJ]] | ||
[[Category: Stachel | [[Category: Steele TG]] | ||
[[Category: Steele | [[Category: Vacca JP]] | ||
[[Category: Vacca | |||
Latest revision as of 10:35, 23 August 2023
Crystal structure of human Beta-secretase complexed with L-L000430,469Crystal structure of human Beta-secretase complexed with L-L000430,469
Structural highlights
FunctionBACE1_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.[1] [2] Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMedWe have synthesized and evaluated a series of conformationally biased P3 amide replacements based on an isophthalamide lead structure. The studies resulted in the identification of the beta-secretase inhibitor 7m which has an in vitro IC(50)=35 nM. The synthesis and biological activities of these compounds are described. Conformationally biased P3 amide replacements of beta-secretase inhibitors.,Stachel SJ, Coburn CA, Steele TG, Crouthamel MC, Pietrak BL, Lai MT, Holloway MK, Munshi SK, Graham SL, Vacca JP Bioorg Med Chem Lett. 2006 Feb;16(3):641-4. Epub 2005 Nov 2. PMID:16263281[3] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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