Hsp90 Inhibitors
Hsp90 is a molecular chaperone responsible for folding denatured
and nascent proteins. Numerous proteins required for cancerous
grwoth are dependent on Hsp90 for their conformational maturation
to a biologically active three-dimensional protein. Inhibition
of Hsp90 results in the simultaneous inhibition of multiple protein
targets. The molecules identified herein are designed to inhibit
Hsp90 and thus prevent the conformational maturation of Hsp90
dependent proteins.
Benefits
Geldanamycin and other known inhibitors of Hsp90 are difficult
to prepare and analogues of such compounds are not likely to
become drugs due to poor solubility and toxicity unrelated to
the inhibition of Hsp90. However, the molecules described herein
are easily assembled and can be rapidly derivatized for the preparation
of numerous analogues with additional potential for increasing
solubility and decreasing toxicity.
Potential Uses
Inhibitors of Hsp90 have been shown to be active against several
cancers and the molecules described herein may have similar potential
to 17-allylaminogeldanamycin, which is currently in Phase I clinical
trials for the treatment of cancer.
Development Status
The molecules described herein represent the first set of new
lead compounds for the inhibition of Hsp90.
Patent: Pending
License: Negotiable
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