2b8v
From Proteopedia
(New page: 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'' |
Revision as of 14:35, 21 February 2008
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Crystal structure of human Beta-secretase complexed with L-L000430,469
Overview
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
2B8V 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
Conformationally biased P3 amide replacements of beta-secretase inhibitors., Stachel SJ, Coburn CA, Steele TG, Crouthamel MC, Pietrak BL, Lai MT, Holloway MK, Munshi SK, Graham SL, Vacca JP, Bioorg Med Chem Lett. 2006 Feb;16(3):641-4. Epub 2005 Nov 2. PMID:16263281
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