Case Study
Targeting STAT3 withSelective Protein Degraders for the Treatment of PTCL Case Study
The activity of Signal Transducer and Activator of Transcription 3 (STAT3) is dysregulated in many cancers including aggressive hematological malignancies with high unmet medical need. Aberrant activation of STAT3 can promote the establishment and progression of malignant cells through regulation of cell survival and proliferation pathways and suppression of anti-tumor immunity, also known as tumor intrinsic and tumor extrinsic mechanisms, respectively. Selective targeting of STAT3 has been challenging, but targeted protein degradation mediated by heterobifunctional small molecule degraders is a novel therapeutic modality to target difficult-to-drug oncogenic proteins. These molecules bind to both the target protein and an E3 ligase, enabling the formation of a ternary complex.