2iqg
From Proteopedia
(New page: 200px<br /> <applet load="2iqg" size="450" color="white" frame="true" align="right" spinBox="true" caption="2iqg, resolution 1.700Å" /> '''Crystal Structure ...) |
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caption="2iqg, resolution 1.700Å" /> | caption="2iqg, resolution 1.700Å" /> | ||
'''Crystal Structure of Hydroxyethyl Secondary Amine-based Peptidomimetic Inhibitor of Human Beta-Secretase (BACE)'''<br /> | '''Crystal Structure of Hydroxyethyl Secondary Amine-based Peptidomimetic Inhibitor of Human Beta-Secretase (BACE)'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2IQG 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 F2I as [http://en.wikipedia.org/wiki/ligand ligand]. 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:// | + | 2IQG 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=F2I:'>F2I</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. 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=2IQG 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 Fri Feb 15 17:36:39 2008'' |
Revision as of 15:36, 15 February 2008
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Crystal Structure of Hydroxyethyl Secondary Amine-based Peptidomimetic Inhibitor of Human Beta-Secretase (BACE)
Overview
The design and synthesis of a novel series of potent and cell permeable, peptidomimetic inhibitors of the human beta-secretase (BACE) are, described. These inhibitors feature a hydroxyethyl secondary amine, isostere and a novel aromatic ring replacement for the C-terminus. The, crystal structure of BACE in complex with this hydroxyethyl secondary, amine isostere inhibitor is also presented.
About this Structure
2IQG is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Memapsin 2, with EC number 3.4.23.46 Full crystallographic information is available from OCA.
Reference
Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human beta-secretase., Maillard MC, Hom RK, Benson TE, Moon JB, Mamo S, Bienkowski M, Tomasselli AG, Woods DD, Prince DB, Paddock DJ, Emmons TL, Tucker JA, Dappen MS, Brogley L, Thorsett ED, Jewett N, Sinha S, John V, J Med Chem. 2007 Feb 22;50(4):776-81. PMID:17300163
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