2bre

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[[Image:2bre.gif|left|200px]]
[[Image:2bre.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2bre |SIZE=350|CAPTION= <scene name='initialview01'>2bre</scene>, resolution 2.0&Aring;
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The line below this paragraph, containing "STRUCTURE_2bre", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Kj2+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=KJ2:4-{4-[4-(3-AMINOPROPOXY)PHENYL]-1H-PYRAZOL-5-YL}-6-CHLOROBENZENE-1,3-DIOL'>KJ2</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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|GENE=
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|DOMAIN=
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{{STRUCTURE_2bre| PDB=2bre | 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=2bre FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2bre OCA], [http://www.ebi.ac.uk/pdbsum/2bre PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2bre RCSB]</span>
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}}
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'''STRUCTURE OF A HSP90 INHIBITOR BOUND TO THE N-TERMINUS OF YEAST HSP90.'''
'''STRUCTURE OF A HSP90 INHIBITOR BOUND TO THE N-TERMINUS OF YEAST HSP90.'''
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[[Category: Roe, S M.]]
[[Category: Roe, S M.]]
[[Category: 3d-structure]]
[[Category: 3d-structure]]
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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: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: multigene family]]
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[[Category: Multigene family]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:41:26 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:10:38 2008''
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Revision as of 17:41, 3 May 2008

Image:2bre.gif

Template:STRUCTURE 2bre

STRUCTURE OF A HSP90 INHIBITOR BOUND TO THE N-TERMINUS OF YEAST HSP90.


Overview

High-throughput screening identified the 3,4-diarylpyrazole CCT018159 as a novel and potent (7.1 microM) inhibitor of Hsp90 ATPase activity. Here, we describe the synthesis of CCT018159 and a number of close analogues together with data on their biochemical properties. Some initial structure-activity relationships are discussed, as well as the crystal structure of CCT018159 bound to Hsp90.

About this Structure

2BRE is a Single protein structure of sequence from Saccharomyces cerevisiae. Full crystallographic information is available from OCA.

Reference

The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors., Cheung KM, Matthews TP, James K, Rowlands MG, Boxall KJ, Sharp SY, Maloney A, Roe SM, Prodromou C, Pearl LH, Aherne GW, McDonald E, Workman P, Bioorg Med Chem Lett. 2005 Jul 15;15(14):3338-43. PMID:15955698 Page seeded by OCA on Sat May 3 20:41:26 2008

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