2p83
From Proteopedia
(New page: 200px<br /> <applet load="2p83" size="450" color="white" frame="true" align="right" spinBox="true" caption="2p83, resolution 2.500Å" /> '''Potent and selecti...) |
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| - | [[Image:2p83. | + | [[Image:2p83.jpg|left|200px]]<br /><applet load="2p83" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="2p83, resolution 2.500Å" /> | caption="2p83, resolution 2.500Å" /> | ||
'''Potent and selective isophthalamide S2 hydroxyethylamine inhibitor of BACE1'''<br /> | '''Potent and selective isophthalamide S2 hydroxyethylamine inhibitor of BACE1'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2P83 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with PO4 and MR0 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http:// | + | 2P83 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=PO4:'>PO4</scene> and <scene name='pdbligand=MR0:'>MR0</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2P83 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: protein-inhibitor complex]] | [[Category: protein-inhibitor complex]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 14:50:21 2008'' |
Revision as of 12:50, 23 January 2008
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Potent and selective isophthalamide S2 hydroxyethylamine inhibitor of BACE1
Overview
The design and synthesis of a novel series of potent BACE1, hydroxyethylamine inhibitors. These inhibitors feature hydrogen bonding, substituents at the C-5 position of the isophthalamide ring with improved, selectivity over cathepsin D.
About this Structure
2P83 is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as Memapsin 2, with EC number 3.4.23.46 Full crystallographic information is available from OCA.
Reference
Potent and selective isophthalamide S(2) hydroxyethylamine inhibitors of BACE1., Kortum SW, Benson TE, Bienkowski MJ, Emmons TL, Prince DB, Paddock DJ, Tomasselli AG, Moon JB, Laborde A, Tenbrink RE, Bioorg Med Chem Lett. 2007 Jun 15;17(12):3378-83. Epub 2007 Apr 3. PMID:17434734
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