The effectiveness of HS-72 variants in inhibition of heat shock protein 72
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Heat shock proteins (HSPs) play important roles in the process of maintaining proteostasis in a cell. HSP72, the inducible form of the HSP70 family, is expressed in response to stress on the cell or tissue, including those stresses caused by tumor growth. Increasing evidence suggests that HSP72 is necessary for a cancerous cell to survive under the stresses of a tumor microenvironment. This has naturally raised interest in identifying an inhibitor selective for HSP72. The Haystead Laboratory at Duke University identified such a small-molecule inhibitor, referred to as HS-72, and proposed the scaffold as an ideal starting point to develop a family of therapeutic agents targeting HSP72. This work examines the potency and effectiveness of HS-72 and a number of its analogs developed by the Haystead Laboratory. These results suggest that HS-159 is a more effective inhibitor of HSP72 on a range of human tumor cell lines than HS-72. Further studies are needed to quantify how much more potent HS-159 is than HS-72 and potentially identify even more potent compounds.