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| - | [[Image:2vls.jpg|left|200px]] | + | #REDIRECT [[2vwc]] This PDB entry is obsolete and replaced by 2vwc |
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| - | {{STRUCTURE_2vls| PDB=2vls | SCENE= }}
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| - | '''STRUCTURE OF THE HSP90 INHIBITOR MACBECIN BOUND TO THE N-TERMINUS OF YEAST HSP90.'''
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| - | ==Overview==
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| - | Macbecin compares favorably to geldanamycin as an Hsp90 inhibitor, being more soluble, stable, more potently inhibiting ATPase activity (IC 50 = 2 microM) and binding with higher affinity ( K d = 0.24 microM). Structural studies reveal significant differences in their Hsp90 binding characteristics, and macbecin-induced tumor cell growth inhibition is accompanied by characteristic degradation of Hsp90 client proteins. Macbecin significantly reduced tumor growth rates (minimum T/ C: 32%) in a DU145 murine xenograft. Macbecin thus represents an attractive lead for further optimization.
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| - | ==About this Structure==
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| - | 2VLS is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Saccharomyces_cerevisiae Saccharomyces cerevisiae]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2VLS OCA].
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| - | ==Reference==
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| - | Molecular Characterization of Macbecin as an Hsp90 Inhibitor., Martin CJ, Gaisser S, Challis IR, Carletti I, Wilkinson B, Gregory M, Prodromou C, Roe SM, Pearl LH, Boyd SM, Zhang MQ, J Med Chem. 2008 Mar 22;. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/18357975 18357975]
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| - | [[Category: Saccharomyces cerevisiae]]
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| - | [[Category: Single protein]]
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| - | [[Category: Pearl, L H.]]
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| - | [[Category: Prodromou, C.]]
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| - | [[Category: Roe, S M.]]
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| - | [[Category: Atp-binding]]
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| - | [[Category: Cell cycle]]
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| - | [[Category: Chaperone]]
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| - | [[Category: Chaperone-complex]]
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| - | [[Category: Chaperone/complex]]
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| - | [[Category: Cytoplasm]]
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| - | [[Category: Heat shock]]
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| - | [[Category: Inhibitor]]
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| - | [[Category: Multigene family]]
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| - | [[Category: Nucleotide-binding]]
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| - | [[Category: Stress response]]
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