Therapeutics: Estrogen receptor α; histone deacetylase (HDAC)

In vitro studies suggest conjugates of the HDAC inhibitor Zolinza vorinostat and analogs of the estrogen receptor α inhibitor oxabicycloheptene sulfonate could help treat breast cancer. Chemical synthesis and in vitro testing of the conjugates identified multiple compounds that inhibited both estrogen receptor α and HDAC with nanomolar IC50 values. In human breast cancer cell lines, the compounds increased cell death compared with tamoxifen. Next steps include examining the most potent compounds in mouse models of breast cancer.

Merck & Co. Inc. and Taiho Pharmaceutical Co. Ltd. market vorinostat to treat cutaneous T cell lymphoma (CTCL)...