2bt0: Difference between revisions
New page: left|200px<br /> <applet load="2bt0" size="450" color="white" frame="true" align="right" spinBox="true" caption="2bt0, resolution 1.90Å" /> '''NOVEL, POTENT SMALL... |
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==About this Structure== | ==About this Structure== | ||
2BT0 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 CT5 as [[http://en.wikipedia.org/wiki/ligand ligand]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2BT0 OCA]]. | 2BT0 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 CT5 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=2BT0 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 14:23:05 2007'' | ||
Revision as of 15:18, 30 October 2007
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NOVEL, POTENT SMALL MOLECULE INHIBITORS OF THE MOLECULAR CHAPERONE HSP90 DISCOVERED THROUGH STRUCTURE-BASED DESIGN
OverviewOverview
The crystal structure of a previously reported screening hit 1 (CCT018159), bound to the N terminal domain of molecular chaperone Hsp90 has been used, to design 5-amide analogues. These exhibit enhanced potency against the, target in binding and functional assays with accompanying appropriate, cellular pharmacodynamic changes. Compound 11 (VER-49009) compares, favorably with the clinically evaluated 17-AAG.
About this StructureAbout this Structure
2BT0 is a [Single protein] structure of sequence from [Homo sapiens] with CT5 as [ligand]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].
ReferenceReference
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design., Dymock BW, Barril X, Brough PA, Cansfield JE, Massey A, McDonald E, Hubbard RE, Surgenor A, Roughley SD, Webb P, Workman P, Wright L, Drysdale MJ, J Med Chem. 2005 Jun 30;48(13):4212-5. PMID:15974572
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