UHRF1 is a key epigenetic regulator implicated in prostate cancer, yet no targeted therapies have reached clinical trials. Here, the authors develop H93, a hybrid small molecule that directly binds the UHRF1 SRA domain and unexpectedly promotes its dimerization, and disrupts its interaction with DNMT1, reactivates silenced tumor suppressors, and confers potent antitumor efficacy in prostate cancer.
- Yuxin Fu
- Longying Jiang
- Xiong Li