2b8v: Difference between revisions
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New page: left|200px<br /> <applet load="2b8v" size="450" color="white" frame="true" align="right" spinBox="true" caption="2b8v, resolution 1.80Å" /> '''Crystal structure o... |
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[[Image:2b8v.gif|left|200px]]<br /> | [[Image:2b8v.gif|left|200px]]<br /><applet load="2b8v" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="2b8v" size=" | |||
caption="2b8v, resolution 1.80Å" /> | caption="2b8v, resolution 1.80Å" /> | ||
'''Crystal structure of human Beta-secretase complexed with L-L000430,469'''<br /> | '''Crystal structure of human Beta-secretase complexed with L-L000430,469'''<br /> | ||
==Overview== | ==Overview== | ||
We have synthesized and evaluated a series of conformationally biased P3 | We have synthesized and evaluated a series of conformationally biased P3 amide replacements based on an isophthalamide lead structure. The studies resulted in the identification of the beta-secretase inhibitor 7m which has an in vitro IC(50)=35 nM. The synthesis and biological activities of these compounds are described. | ||
==About this Structure== | ==About this Structure== | ||
2B8V 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 3BN 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:// | 2B8V 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=3BN:'>3BN</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=2B8V OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Memapsin 2]] | [[Category: Memapsin 2]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Coburn, C | [[Category: Coburn, C A.]] | ||
[[Category: Crouthamel, M | [[Category: Crouthamel, M C.]] | ||
[[Category: Graham, S | [[Category: Graham, S L.]] | ||
[[Category: Holloway, M | [[Category: Holloway, M K.]] | ||
[[Category: Lai, M | [[Category: Lai, M T.]] | ||
[[Category: Munshi, S | [[Category: Munshi, S K.]] | ||
[[Category: Pietrak, B | [[Category: Pietrak, B L.]] | ||
[[Category: Stachel, S | [[Category: Stachel, S J.]] | ||
[[Category: Steele, T | [[Category: Steele, T G.]] | ||
[[Category: Vacca, J | [[Category: Vacca, J P.]] | ||
[[Category: 3BN]] | [[Category: 3BN]] | ||
[[Category: aspartyl protease]] | [[Category: aspartyl protease]] | ||
[[Category: bace]] | [[Category: bace]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:35:19 2008'' | ||
