2bt0: Difference between revisions
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{{STRUCTURE_2bt0| PDB=2bt0 | SCENE= }} | |||
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'''NOVEL, POTENT SMALL MOLECULE INHIBITORS OF THE MOLECULAR CHAPERONE HSP90 DISCOVERED THROUGH STRUCTURE-BASED DESIGN''' | '''NOVEL, POTENT SMALL MOLECULE INHIBITORS OF THE MOLECULAR CHAPERONE HSP90 DISCOVERED THROUGH STRUCTURE-BASED DESIGN''' | ||
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[[Category: Workman, P.]] | [[Category: Workman, P.]] | ||
[[Category: Wright, L.]] | [[Category: Wright, L.]] | ||
[[Category: | [[Category: Atp-binding]] | ||
[[Category: | [[Category: Chaperone]] | ||
[[Category: | [[Category: Heat shock]] | ||
[[Category: | [[Category: Phosphorylation]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:45:29 2008'' | |||
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Revision as of 20:45, 3 May 2008
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. 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 Page seeded by OCA on Sat May 3 20:45:29 2008