2bsm
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(New page: 200px<br /> <applet load="2bsm" size="450" color="white" frame="true" align="right" spinBox="true" caption="2bsm, resolution 2.05Å" /> '''NOVEL, POTENT SMALL...)
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Revision as of 17:30, 29 October 2007
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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]. 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
Page seeded by OCA on Mon Oct 29 19:35:04 2007
Categories: Homo sapiens | Single protein | Barril, X. | Brough, P.A. | Cansfield, J.E. | Drysdale, M.J. | Dymock, B.W. | Hubbard, R.E. | Massey, A. | Mcdonald, E. | Roughley, S.D. | Surgenor, A. | Webb, P. | Workman, P. | Wright, L. | BSM | Atp-binding | Atpase | Chaperone | Heat shock | Hsp90 | Pu3
