An Apoptosis‐Inducing Small Molecule That Binds to Heat Shock Protein 70

Abstract

A cell-based screening approach in which annexin V was used as a staining agent identified apoptozole (Az; see scheme) as an imidazole-based molecule which induces apoptosis. Az binds to Hsc70 and Hsp70 (anti-apoptotic chaperone proteins), with dissociation constants of 0.21 and 0.14 μM, respectively, thereby inhibiting their function. Thus, Az possesses antitumor activity and is, therefore, a potential cancer therapeutic agent. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2008/z802801_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.