2bsm

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[[Image:2bsm.gif|left|200px]]
[[Image:2bsm.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2bsm |SIZE=350|CAPTION= <scene name='initialview01'>2bsm</scene>, resolution 2.05&Aring;
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The line below this paragraph, containing "STRUCTURE_2bsm", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Bsm+Binding+Site+For+Chain+A'>AC1</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=BSM:5-(5-CHLORO-2,4-DIHYDROXYPHENYL)-N-ETHYL-4-(4-METHOXYPHENYL)-1H-PYRAZOLE-3-CARBOXAMIDE'>BSM</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_2bsm| PDB=2bsm | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2bsm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2bsm OCA], [http://www.ebi.ac.uk/pdbsum/2bsm PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2bsm RCSB]</span>
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}}
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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.]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: atpase]]
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[[Category: Atpase]]
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[[Category: chaperone]]
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[[Category: Chaperone]]
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[[Category: heat shock]]
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[[Category: Heat shock]]
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[[Category: hsp90]]
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[[Category: Hsp90]]
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[[Category: pu3]]
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[[Category: Pu3]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:44:43 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:11:11 2008''
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Revision as of 17:44, 3 May 2008

Image:2bsm.gif

Template:STRUCTURE 2bsm

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. 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 Sat May 3 20:44:43 2008

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