SF-3-030: A Function-Selective ERK2 Inhibitor for Targeted Cancer Therapy

The content of this video is based on Mol Carcinog's publication of Passaniti et al., 2022 "Targeting mitochondrial metabolism for metastatic cancer therapy".
Key Takeaways:
✅ SF-3-030 is a function-selective ERK2 inhibitor targeting the F-recruitment site (FRS) instead of the ATP-binding site.
✅ Selective C252 modification disrupts oncogenic ERK signaling while preserving normal kinase activity.
✅ Reduces toxicity and off-target effects compared to traditional ATP-competitive inhibitors.
✅ Potential therapeutic application in ERK-driven cancers (e.g., melanoma, lung cancer).
✅ Future research will focus on combination therapies with BRAF and MEK inhibitors to overcome resistance.
✅ A promising strategy for safer and more precise cancer treatment.
Final Thought:
SF-3-030 highlights the power of targeting protein-protein interactions in drug development, paving the way for next-generation cancer therapies with improved efficacy and safety.