2bz5
From Proteopedia
(New page: 200px<br /> <applet load="2bz5" size="450" color="white" frame="true" align="right" spinBox="true" caption="2bz5, resolution 1.90Å" /> '''STRUCTURE-BASED DIS...) |
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==About this Structure== | ==About this Structure== | ||
| - | 2BZ5 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 AB4 as [[http://en.wikipedia.org/wiki/ligand ligand]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2BZ5 OCA]]. | + | 2BZ5 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 AB4 as [[http://en.wikipedia.org/wiki/ligand ligand]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2BZ5 OCA]]. |
==Reference== | ==Reference== | ||
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[[Category: phosphorylation]] | [[Category: phosphorylation]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 12:31:03 2007'' |
Revision as of 10:26, 30 October 2007
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STRUCTURE-BASED DISCOVERY OF A NEW CLASS OF HSP90 INHIBITORS
Overview
Docking-based virtual screening identified 1-(2-phenol)-2-naphthol, compounds as a new class of Hsp90 inhibitors of low to sub-micromolar, potency. Here we report the binding affinities and cellular activities of, several members of this class. A high resolution crystal structure of the, most potent compound reveals its binding mode in the ATP binding site of, Hsp90, providing a rationale for the observed activity of the series and, suggesting strategies for developing compounds with improved properties.
About this Structure
2BZ5 is a [Single protein] structure of sequence from [Homo sapiens] with AB4 as [ligand]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].
Reference
Structure-based discovery of a new class of Hsp90 inhibitors., Barril X, Brough P, Drysdale M, Hubbard RE, Massey A, Surgenor A, Wright L, Bioorg Med Chem Lett. 2005 Dec 1;15(23):5187-91. Epub 2005 Oct 3. PMID:16202589
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