2bt0

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[[Image:2bt0.gif|left|200px]]
[[Image:2bt0.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2bt0 |SIZE=350|CAPTION= <scene name='initialview01'>2bt0</scene>, resolution 1.90&Aring;
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The line below this paragraph, containing "STRUCTURE_2bt0", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Ct5+Binding+Site+For+Chain+B'>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=CT5:4-[4-(2,3-DIHYDRO-1,4-BENZODIOXIN-6-YL)-3-METHYL-1H-PYRAZOL-5-YL]-6-ETHYLBENZENE-1,3-DIOL'>CT5</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_2bt0| PDB=2bt0 | 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=2bt0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2bt0 OCA], [http://www.ebi.ac.uk/pdbsum/2bt0 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2bt0 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: 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: phosphorylation]]
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[[Category: Phosphorylation]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:45:29 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:11:23 2008''
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Revision as of 17:45, 3 May 2008

Image:2bt0.gif

Template:STRUCTURE 2bt0

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

2BT0 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 20:45:29 2008

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OCA

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