3ckp: Difference between revisions
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==Crystal structure of BACE-1 in complex with inhibitor== | ==Crystal structure of BACE-1 in complex with inhibitor== | ||
<StructureSection load='3ckp' size='340' side='right' caption='[[3ckp]], [[Resolution|resolution]] 2.30Å' scene=''> | <StructureSection load='3ckp' size='340' side='right' caption='[[3ckp]], [[Resolution|resolution]] 2.30Å' scene=''> | ||
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3ckr|3ckr]]</td></tr> | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3ckr|3ckr]]</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=3ckp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ckp OCA], [http://pdbe.org/3ckp PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3ckp RCSB], [http://www.ebi.ac.uk/pdbsum/3ckp 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=3ckp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ckp OCA], [http://pdbe.org/3ckp PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3ckp RCSB], [http://www.ebi.ac.uk/pdbsum/3ckp PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3ckp ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
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</div> | </div> | ||
<div class="pdbe-citations 3ckp" style="background-color:#fffaf0;"></div> | <div class="pdbe-citations 3ckp" style="background-color:#fffaf0;"></div> | ||
== References == | == References == | ||
<references/> | <references/> | ||
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[[Category: Memapsin 2]] | [[Category: Memapsin 2]] | ||
[[Category: Min, K]] | [[Category: Min, K]] | ||
[[Category: Alternative splicing]] | |||
[[Category: Aspartyl protease]] | [[Category: Aspartyl protease]] | ||
[[Category: Beta-secretase]] | [[Category: Beta-secretase]] | ||
Revision as of 11:29, 25 October 2017
Crystal structure of BACE-1 in complex with inhibitorCrystal structure of BACE-1 in complex with inhibitor
Structural highlights
Function[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.[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 describe synthesis and evaluation of a series of cyclic urea derivatives with hydroxylethylamine isostere. Modification of P3, P1, and P2' and combination of SAR display a >100-fold increase in potency with good cellular activity (IC(50)=0.15microM) relative to the previously reported compound 3. Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives.,Park H, Min K, Kwak HS, Koo KD, Lim D, Seo SW, Choi JU, Platt B, Choi DY Bioorg Med Chem Lett. 2008 May 1;18(9):2900-4. Epub 2008 Apr 8. PMID:18434152[3] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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