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2oah

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(New page: 200px<br /> <applet load="2oah" size="450" color="white" frame="true" align="right" spinBox="true" caption="2oah, resolution 1.80&Aring;" /> '''Crystal Structure o...)
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[[Image:2oah.gif|left|200px]]<br />
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[[Image:2oah.jpg|left|200px]]<br /><applet load="2oah" size="350" color="white" frame="true" align="right" spinBox="true"
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<applet load="2oah" size="450" color="white" frame="true" align="right" spinBox="true"
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caption="2oah, resolution 1.80&Aring;" />
caption="2oah, resolution 1.80&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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2OAH 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 QIN 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://ispc.weizmann.ac.il/oca-bin/ocashort?id=2OAH OCA].
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2OAH 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=QIN:'>QIN</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=2OAH 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 23:08:18 2007''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:49:31 2008''

Revision as of 10:49, 23 January 2008

Image:2oah.jpg

2oah, resolution 1.80Å

Drag the structure with the mouse to rotate

Crystal Structure of Human Beta Secretase Complexed with inhibitor

Overview

A series of low-molecular weight 2,6-diamino-isonicotinamide BACE-1, inhibitors containing an amine transition-state isostere were synthesized, and shown to be highly potent in both enzymatic and cell-based assays., These inhibitors contain a trans-S,S-methyl cyclopropane P(3) which bind, BACE-1 in a 10s-loop down conformation giving rise to highly potent, compounds with favorable molecular weight and moderate to high, susceptibility to P-glycoprotein (P-gp) efflux.

About this Structure

2OAH 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

Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation., Stauffer SR, Stanton MG, Gregro AR, Steinbeiser MA, Shaffer JR, Nantermet PG, Barrow JC, Rittle KE, Collusi D, Espeseth AS, Lai MT, Pietrak BL, Holloway MK, McGaughey GB, Munshi SK, Hochman JH, Simon AJ, Selnick HG, Graham SL, Vacca JP, Bioorg Med Chem Lett. 2007 Mar 15;17(6):1788-92. Epub 2006 Dec 21. PMID:17257835

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