2xjj

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[[Image:2xjj.png|left|200px]]
 
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{{STRUCTURE_2xjj| PDB=2xjj | SCENE= }}
{{STRUCTURE_2xjj| PDB=2xjj | SCENE= }}
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===Structure of HSP90 with small molecule inhibitor bound===
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{{ABSTRACT_PUBMED_20662534}}
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===STRUCTRE OF HSP90 WITH SMALL MOLECULE INHIBITOR BOUND===
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==Function==
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[[http://www.uniprot.org/uniprot/HS90A_HUMAN HS90A_HUMAN]] Molecular chaperone that promotes the maturation, structural maintenance and proper regulation of specific target proteins involved for instance in cell cycle control and signal transduction. Undergoes a functional cycle that is linked to its ATPase activity. This cycle probably induces conformational changes in the client proteins, thereby causing their activation. Interacts dynamically with various co-chaperones that modulate its substrate recognition, ATPase cycle and chaperone function.<ref>PMID:15937123</ref> <ref>PMID:11274138</ref>
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{{ABSTRACT_PUBMED_20662534}}
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==About this Structure==
==About this Structure==
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==Reference==
==Reference==
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<ref group="xtra">PMID:020662534</ref><references group="xtra"/>
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<ref group="xtra">PMID:020662534</ref><references group="xtra"/><references/>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Callaghan, O.]]
[[Category: Callaghan, O.]]
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[[Category: Frederickson, M.]]
[[Category: Frederickson, M.]]
[[Category: Graham, B.]]
[[Category: Graham, B.]]
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[[Category: Mcmenamin, R.]]
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[[Category: McMenamin, R.]]
[[Category: Murray, C W.]]
[[Category: Murray, C W.]]
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[[Category: Obrien, M A.]]
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[[Category: OBrien, M A.]]
[[Category: Patel, S.]]
[[Category: Patel, S.]]
[[Category: Phillips, T R.]]
[[Category: Phillips, T R.]]

Revision as of 09:21, 24 April 2013

Template:STRUCTURE 2xjj

Contents

Structure of HSP90 with small molecule inhibitor bound

Template:ABSTRACT PUBMED 20662534

Function

[HS90A_HUMAN] Molecular chaperone that promotes the maturation, structural maintenance and proper regulation of specific target proteins involved for instance in cell cycle control and signal transduction. Undergoes a functional cycle that is linked to its ATPase activity. This cycle probably induces conformational changes in the client proteins, thereby causing their activation. Interacts dynamically with various co-chaperones that modulate its substrate recognition, ATPase cycle and chaperone function.[1] [2]

About this Structure

2xjj is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

See Also

Reference

  • Woodhead AJ, Angove H, Carr MG, Chessari G, Congreve M, Coyle JE, Cosme J, Graham B, Day PJ, Downham R, Fazal L, Feltell R, Figueroa E, Frederickson M, Lewis J, McMenamin R, Murray CW, O'Brien MA, Parra L, Patel S, Phillips T, Rees DC, Rich S, Smith DM, Trewartha G, Vinkovic M, Williams B, Woolford AJ. Discovery of (2,4-Dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-di hydroisoindol-2-yl]methanone (AT13387), a Novel Inhibitor of the Molecular Chaperone Hsp90 by Fragment Based Drug Design. J Med Chem. 2010 Jul 28. PMID:20662534 doi:10.1021/jm100060b
  1. ↑ Martinez-Ruiz A, Villanueva L, Gonzalez de Orduna C, Lopez-Ferrer D, Higueras MA, Tarin C, Rodriguez-Crespo I, Vazquez J, Lamas S. S-nitrosylation of Hsp90 promotes the inhibition of its ATPase and endothelial nitric oxide synthase regulatory activities. Proc Natl Acad Sci U S A. 2005 Jun 14;102(24):8525-30. Epub 2005 Jun 3. PMID:15937123 doi:10.1073/pnas.0407294102
  2. ↑ Forsythe HL, Jarvis JL, Turner JW, Elmore LW, Holt SE. Stable association of hsp90 and p23, but Not hsp70, with active human telomerase. J Biol Chem. 2001 May 11;276(19):15571-4. Epub 2001 Mar 23. PMID:11274138 doi:10.1074/jbc.C100055200

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