Award Details:
Award Type: Accelerator
Award #: A-009
Proposal Title: A Novel BET Inhibitor for Breast Cancer Combination Therapy
PI(s): Gregory Thatcher (UIC)
Award Amount: $100,000.00
Application Cycle: Round 2 (Fall 2018)
Award Start Date: January 1, 2019
Award End Date: December 31, 2019
Abstract:
Deregulation of epigenetic processes is one of the hallmarks of cancer. Bromodomain-containing proteins are key epigenetic regulators: among 61 bromodomains, the bromodomain and extra- terminal (BET) family has been targeted by inhibitors in cancer clinical trials. We have designed a novel, potent, selective BET inhibitor, YF-2-23, with superiority to many inhibitors in clinical trials, when tested in breast cancer cell lines. Although YF-2-23 may have use in multiple cancers, a persuasive argument exists for pursuing combination therapy in drug-resistant ER+ breast cancer, with a novel, proprietary, orally bioavailable selective estrogen receptor degrader (SERD). We propose to obtain crucial preclinical efficacy data on the YF-2-23 combination in xenograft models of metastatic ER+ breast cancer, resistant to endocrine therapy and CDK4/6 inhibitors.