2iqg
From Proteopedia
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==Overview== | ==Overview== | ||
| - | The design and synthesis of a novel series of potent and cell permeable | + | 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== | ==About this Structure== | ||
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[[Category: Memapsin 2]] | [[Category: Memapsin 2]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Benson, T | + | [[Category: Benson, T E.]] |
| - | [[Category: Emmons, T | + | [[Category: Emmons, T L.]] |
| - | [[Category: Prince, D | + | [[Category: Prince, D B.]] |
| - | [[Category: Tomasselli, A | + | [[Category: Tomasselli, A G.]] |
| - | [[Category: Woods, D | + | [[Category: Woods, D D.]] |
[[Category: F2I]] | [[Category: F2I]] | ||
[[Category: protein-inhibitor complex]] | [[Category: protein-inhibitor complex]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:55:04 2008'' |
Revision as of 15:55, 21 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
Page seeded by OCA on Thu Feb 21 17:55:04 2008
