Cancer

Cell culture and mouse studies identified a naphthalenone-based Hsp90 inhibitor that could help treat glioblastoma. Screening of a small molecule library in a HeLa cell-based activity assay, followed by optimization and in vitro testing of the top hit, yielded a naphthalenone-based compound that inhibited Hsp90 with an IC₅₀ of 29.5 nM. In a human glioblastoma cell line, the compound decreased growth and motility and increased levels of apoptotic markers compared with vehicle. In a xenograft mouse model of glioblastoma, the compound decreased tumor growth. Next steps could include testing the compound in patient-derived xenograft (PDX) mouse model of glioblastoma.

Soligenix Inc. has hypericin, a topical phototherapeutic agent that inhibits Hsp90, in Phase III testing for cutaneous T cell lymphoma (CTCL)...