In the last decade, the molecular chaperone HSP90 has emerged as an important target in cancer therapeutics
and has subsequently become the focus of several drug discovery and development efforts. The first-in-class HSP90 inhibitor
17-AAG entered into Phase I clinical trial in 1999. Today 13 HSP90 inhibitors representing multiple drug classes,
with different modes of action, are undergoing clinical evaluation. The present review will highlight the involvement of
HSP90 in regulating and maintaining the transformed phenotype, provide an overview on current HSP90 inhibitors and
further update on the most relevant patents which have recently appeared in the literature.
Keywords: Cancer therapeutics, cell surface, chaperoning, drug discovery, HSP90, signal transduction.
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