Targeting the cancer chaperone HSP90

Through its chaperoning activity, HSP90 is a master regulator of many cancer-associated proteins. Inhibitors of HSP90 exhibit the unique ability to disrupt oncogenic signalling networks at multiple levels. With the first inhibitors now in phase II clinical trials, the results have so far been encouraging, prompting the creation of a second generation of inhibitors. Here, we review the progress made with current and emerging HSP90 inhibitors. We also describe our present understanding of their mechanisms of action and highlight potential new approaches to modulate HSP90 for cancer treatment.

Section editors:Victoria Heath and Roy Bicknell – University of Birmingham, Institute for Biomedical Research, The Medical School, Edgbaston, Birmingham B15 2TT, UK