4b1e

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==New Aminoimidazoles as BACE-1 Inhibitors: From Rational Design to Ab- lowering in Brain==
==New Aminoimidazoles as BACE-1 Inhibitors: From Rational Design to Ab- lowering in Brain==
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<StructureSection load='4b1e' size='340' side='right' caption='[[4b1e]], [[Resolution|resolution]] 1.95&Aring;' scene=''>
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<StructureSection load='4b1e' size='340' side='right'caption='[[4b1e]], [[Resolution|resolution]] 1.95&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4b1e]] 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=4B1E OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4B1E FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4b1e]] 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=4B1E OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4B1E 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=6T6:(2R)-2-METHYL-5-PHENYL-2-(3-PYRIDIN-3-YLPHENYL)-2,3-DIHYDRO-1H-IMIDAZOL-4-AMINE'>6T6</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.95&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1fkn|1fkn]], [[1m4h|1m4h]], [[1py1|1py1]], [[1sgz|1sgz]], [[1tqf|1tqf]], [[1ujj|1ujj]], [[1ujk|1ujk]], [[1w50|1w50]], [[1w51|1w51]], [[1xn2|1xn2]], [[1xn3|1xn3]], [[1xs7|1xs7]], [[1ym2|1ym2]], [[1ym4|1ym4]], [[2b8l|2b8l]], [[2b8v|2b8v]], [[2fdp|2fdp]], [[2va5|2va5]], [[2va6|2va6]], [[2va7|2va7]], [[2vie|2vie]], [[2vij|2vij]], [[2viy|2viy]], [[2viz|2viz]], [[2vj6|2vj6]], [[2vj7|2vj7]], [[2vj9|2vj9]], [[2vkm|2vkm]], [[2vnm|2vnm]], [[2vnn|2vnn]], [[2wez|2wez]], [[2wf0|2wf0]], [[2wf1|2wf1]], [[2wf2|2wf2]], [[2wf3|2wf3]], [[2wf4|2wf4]], [[2wjo|2wjo]], [[2xfi|2xfi]], [[2xfj|2xfj]], [[2xfk|2xfk]], [[4acu|4acu]], [[4acx|4acx]], [[4azy|4azy]], [[4b00|4b00]], [[4b05|4b05]], [[4b0q|4b0q]], [[4b1c|4b1c]], [[4b1d|4b1d]]</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6T6:(2R)-2-METHYL-5-PHENYL-2-(3-PYRIDIN-3-YLPHENYL)-2,3-DIHYDRO-1H-IMIDAZOL-4-AMINE'>6T6</scene></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'>[https://proteopedia.org/fgij/fg.htm?mol=4b1e FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4b1e OCA], [https://pdbe.org/4b1e PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4b1e RCSB], [https://www.ebi.ac.uk/pdbsum/4b1e PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4b1e ProSAT]</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=4b1e FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4b1e OCA], [http://pdbe.org/4b1e PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4b1e RCSB], [http://www.ebi.ac.uk/pdbsum/4b1e PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4b1e ProSAT]</span></td></tr>
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</table>
</table>
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== 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>
 
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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==See Also==
==See Also==
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*[[Beta secretase|Beta secretase]]
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*[[Beta secretase 3D structures|Beta secretase 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
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[[Category: Homo sapiens]]
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[[Category: Memapsin 2]]
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[[Category: Large Structures]]
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[[Category: Berg, S]]
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[[Category: Blid J]]
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[[Category: Blid, J]]
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[[Category: Eketjall S]]
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[[Category: Eketjall, S]]
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[[Category: Falting J]]
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[[Category: Falting, J]]
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[[Category: Ginman T]]
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[[Category: Ginman, T]]
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[[Category: Gravenfors Y]]
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[[Category: Gravenfors, Y]]
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[[Category: Janson J]]
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[[Category: Janson, J]]
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[[Category: Jeppsson F]]
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[[Category: Jeppsson, F]]
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[[Category: Johansson P]]
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[[Category: Johansson, P]]
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[[Category: Karlstrom S]]
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[[Category: Karlstrom, S]]
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[[Category: Kihlstrom J]]
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[[Category: Kieseritzky, F]]
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[[Category: Kolmodin K]]
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[[Category: Kihlstrom, J]]
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[[Category: Lindstrom J]]
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[[Category: Kolmodin, K]]
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[[Category: Olsson L]]
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[[Category: Lindstrom, J]]
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[[Category: Rahm F]]
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[[Category: Olsson, L]]
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[[Category: Slivo C]]
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[[Category: Rahm, F]]
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[[Category: Stromberg K]]
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[[Category: Slivo, C]]
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[[Category: Swahn B]]
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[[Category: Stromberg, K]]
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[[Category: Viklund J]]
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[[Category: Swahn, B]]
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[[Category: Von Berg S]]
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[[Category: Viklund, J]]
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[[Category: Von Kieseritzky F]]
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[[Category: Hydrolase]]
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[[Category: Structure-based drug design]]
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Current revision

New Aminoimidazoles as BACE-1 Inhibitors: From Rational Design to Ab- lowering in Brain

PDB ID 4b1e

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