2ph6

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(New page: 200px<br /> <applet load="2ph6" size="450" color="white" frame="true" align="right" spinBox="true" caption="2ph6, resolution 2.00&Aring;" /> '''Crystal Structure o...)
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[[Image:2ph6.gif|left|200px]]<br />
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[[Image:2ph6.jpg|left|200px]]<br /><applet load="2ph6" size="350" color="white" frame="true" align="right" spinBox="true"
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<applet load="2ph6" size="450" color="white" frame="true" align="right" spinBox="true"
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caption="2ph6, resolution 2.00&Aring;" />
caption="2ph6, resolution 2.00&Aring;" />
'''Crystal Structure of Human Beta Secretase Complexed with inhibitor'''<br />
'''Crystal Structure of Human Beta Secretase Complexed with inhibitor'''<br />
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==About this Structure==
==About this Structure==
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2PH6 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 SO4 and 712 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://ispc.weizmann.ac.il/oca-bin/ocashort?id=2PH6 OCA].
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2PH6 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=SO4:'>SO4</scene> and <scene name='pdbligand=712:'>712</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=2PH6 OCA].
==Reference==
==Reference==
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[[Category: hydrolase]]
[[Category: hydrolase]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 23:23:49 2007''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:41:14 2008''

Revision as of 10:41, 23 January 2008

Image:2ph6.jpg

2ph6, resolution 2.00Å

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Crystal Structure of Human Beta Secretase Complexed with inhibitor

Overview

This Letter describes the design and synthesis of tertiary carbinamine, macrocyclic inhibitors of the beta-secretase (BACE-1) enzyme. These, macrocyclic inhibitors, some of which incorporate novel P2 substituents, display a 2- to 100-fold increase in potency relative to the previously, described acyclic analogs while affording greater stability.

About this Structure

2PH6 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, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors., Lindsley SR, Moore KP, Rajapakse HA, Selnick HG, Young MB, Zhu H, Munshi S, Kuo L, McGaughey GB, Colussi D, Crouthamel MC, Lai MT, Pietrak B, Price EA, Sankaranarayanan S, Simon AJ, Seabrook GR, Hazuda DJ, Pudvah NT, Hochman JH, Graham SL, Vacca JP, Nantermet PG, Bioorg Med Chem Lett. 2007 Apr 27;. PMID:17482814

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