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J Med Chem. 2008 May 8;51(9):2853-7. doi: 10.1021/jm701558c. Epub 2008 Mar 22.

Molecular characterization of macbecin as an Hsp90 inhibitor.

Author information

  • 1Biotica Technology Limited, Chesterford Research Park, Essex CB10 1XL, U.K. christine.martin@biotica.com

Abstract

Macbecin compares favorably to geldanamycin as an Hsp90 inhibitor, being more soluble, stable, more potently inhibiting ATPase activity (IC50 = 2 microM) and binding with higher affinity (Kd = 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.

PMID:
18357975
[PubMed - indexed for MEDLINE]
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