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5clm

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Current revision (12:13, 14 June 2023) (edit) (undo)
 
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<StructureSection load='5clm' size='340' side='right'caption='[[5clm]], [[Resolution|resolution]] 2.61&Aring;' scene=''>
<StructureSection load='5clm' size='340' side='right'caption='[[5clm]], [[Resolution|resolution]] 2.61&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[5clm]] is a 1 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=5CLM OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5CLM FirstGlance]. <br>
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<table><tr><td colspan='2'>[[5clm]] 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=5CLM OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5CLM FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=52K:N-{3-[(3R)-5-AMINO-3-METHYL-3,6-DIHYDRO-2H-1,4-OXAZIN-3-YL]PHENYL}-5-CHLOROPYRIDINE-2-CARBOXAMIDE'>52K</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</scene></td></tr>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=52K:N-{3-[(3R)-5-AMINO-3-METHYL-3,6-DIHYDRO-2H-1,4-OXAZIN-3-YL]PHENYL}-5-CHLOROPYRIDINE-2-CARBOXAMIDE'>52K</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</scene></td></tr>
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<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>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5clm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5clm OCA], [https://pdbe.org/5clm PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5clm RCSB], [https://www.ebi.ac.uk/pdbsum/5clm PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5clm ProSAT]</span></td></tr>
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<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>
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<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=5clm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5clm OCA], [http://pdbe.org/5clm PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5clm RCSB], [http://www.ebi.ac.uk/pdbsum/5clm PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5clm ProSAT]</span></td></tr>
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</table>
</table>
== Function ==
== Function ==
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[[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>
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[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 ==
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
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[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Memapsin 2]]
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[[Category: Alexander R]]
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[[Category: Alexander, R]]
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[[Category: Alonso De Diego S]]
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[[Category: Alonso, J M]]
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[[Category: Alonso JM]]
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[[Category: Austin, N]]
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[[Category: Austin N]]
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[[Category: Borghys, H]]
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[[Category: Borghys H]]
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[[Category: Brandt, S Van]]
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[[Category: De Cleyn M]]
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[[Category: Cleyn, M De]]
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[[Category: Delgado O]]
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[[Category: Delgado, O]]
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[[Category: Garcia-Molina A]]
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[[Category: Diego, S Alonso De]]
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[[Category: Gijsen H]]
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[[Category: Garcia-Molina, A]]
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[[Category: MacDonald G]]
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[[Category: Gijsen, H]]
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[[Category: Martinez Lamenca C]]
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[[Category: Gool, M Van]]
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[[Category: Moechars D]]
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[[Category: Lamenca, C Martinez]]
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[[Category: Oehlrich D]]
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[[Category: MacDonald, G]]
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[[Category: Prokopcova H]]
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[[Category: Moechars, D]]
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[[Category: Rombouts F]]
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[[Category: Oehlrich, D]]
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[[Category: Surkyn M]]
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[[Category: Prokopcova, H]]
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[[Category: Trabanco A]]
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[[Category: Rombouts, F]]
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[[Category: Tresadern G]]
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[[Category: Surkyn, M]]
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[[Category: Van Brandt S]]
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[[Category: Trabanco, A]]
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[[Category: Van Gool M]]
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[[Category: Tresadern, G]]
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[[Category: Vos A]]
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[[Category: Vos, A]]
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[[Category: Bace1 protease inhibitor]]
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[[Category: Brain penetrant]]
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[[Category: Hydrolase]]
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[[Category: Orally bioavailable]]
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[[Category: Proteros biostructures gmbh]]
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Current revision

1,4-Oxazine BACE1 inhibitors

PDB ID 5clm

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