HSP90-targeted photosensitizer HS-201

A conjugate consisting of a heat shock protein 90 (Hsp90) inhibitor connected via a linker to verteporfin, a photosensitizing agent, with potential imaging, photodynamic and antineoplastic activities. Upon administration, the Hsp90 inhibitor moiety of HS-201 selectively binds to the Hsp90 ATP binding domain in tumor cells and HS-201 accumulates in tumor cells. The verteporfin moiety of HS-201 allows for visualization and photodynamic therapy of the tumors. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins. Verteporfin is a synthetic photosensitizer with photodynamic activity.