2bre

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[[Image:2bre.gif|left|200px]]
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{{Seed}}
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{{STRUCTURE_2bre| PDB=2bre | SCENE= }}
{{STRUCTURE_2bre| PDB=2bre | SCENE= }}
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'''STRUCTURE OF A HSP90 INHIBITOR BOUND TO THE N-TERMINUS OF YEAST HSP90.'''
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===STRUCTURE OF A HSP90 INHIBITOR BOUND TO THE N-TERMINUS OF YEAST HSP90.===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 15955698 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15955698}}
==About this Structure==
==About this Structure==
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[[Category: Inhibitor]]
[[Category: Inhibitor]]
[[Category: Multigene family]]
[[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 Tue Jul 29 04:46:31 2008''

Revision as of 01:46, 29 July 2008

Image:2bre.png

Template:STRUCTURE 2bre

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

Template:ABSTRACT PUBMED 15955698

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 Tue Jul 29 04:46:31 2008

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