2bsm

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==About this Structure==
==About this Structure==
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2BSM 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 BSM 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=2BSM OCA]].
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2BSM 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 BSM 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=2BSM OCA].
==Reference==
==Reference==
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[[Category: pu3]]
[[Category: pu3]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 16:47:03 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 14:09:04 2007''

Revision as of 12:03, 5 November 2007

Image:2bsm.gif

2bsm, resolution 2.05Å

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NOVEL, POTENT SMALL MOLECULE INHIBITORS OF THE MOLECULAR CHAPERONE HSP90 DISCOVERED THROUGH STRUCTURE-BASED DESIGN

Overview

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 Structure

2BSM is a Single protein structure of sequence from Homo sapiens with BSM as ligand. Structure known Active Site: AC1. Full crystallographic information is available from OCA.

Reference

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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