2hiz

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==Overview==
==Overview==
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We describe a novel series of potent inhibitors of human beta-secretase., These compounds possess the hydroxyethyl amine transition state isostere., A 2.5A crystal structure of inhibitor 32 bound to BACE is provided.
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We describe a novel series of potent inhibitors of human beta-secretase. These compounds possess the hydroxyethyl amine transition state isostere. A 2.5A crystal structure of inhibitor 32 bound to BACE is provided.
==About this Structure==
==About this Structure==
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[[Category: Memapsin 2]]
[[Category: Memapsin 2]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: Benson, T.E.]]
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[[Category: Benson, T E.]]
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[[Category: Emmons, T.L.]]
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[[Category: Emmons, T L.]]
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[[Category: Paddock, D.J.]]
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[[Category: Paddock, D J.]]
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[[Category: Prince, D.B.]]
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[[Category: Prince, D B.]]
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[[Category: Tomasselli, A.G.]]
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[[Category: Tomasselli, A G.]]
[[Category: LIJ]]
[[Category: LIJ]]
[[Category: PO4]]
[[Category: PO4]]
[[Category: protein-inhibitor complex]]
[[Category: protein-inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 17:32:25 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:42:26 2008''

Revision as of 15:42, 21 February 2008


2hiz, resolution 2.500Å

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Crystal Structure of human beta-secretase (BACE) in the presence of an inhibitor

Overview

We describe a novel series of potent inhibitors of human beta-secretase. These compounds possess the hydroxyethyl amine transition state isostere. A 2.5A crystal structure of inhibitor 32 bound to BACE is provided.

About this Structure

2HIZ 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

Design of potent inhibitors of human beta-secretase. Part 1., Freskos JN, Fobian YM, Benson TE, Bienkowski MJ, Brown DL, Emmons TL, Heintz R, Laborde A, McDonald JJ, Mischke BV, Molyneaux JM, Moon JB, Mullins PB, Bryan Prince D, Paddock DJ, Tomasselli AG, Winterrowd G, Bioorg Med Chem Lett. 2007 Jan 1;17(1):73-7. Epub 2006 Oct 4. PMID:17046251

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