Structure-Guided Drug Design of MTA-Cooperative PRMT5 Inhibitors
Time: 8:30 am
day: Day 1
Details:
- Highlight rationale for targeting MTA-bound PRMT5 in MTAP-deleted cancers
- Describe efforts informed by structure to convert SAM-cooperative PRMT5 inhibitors to MTA-cooperative PRMT5 inhibitors
- Highlight role of structural biology during efforts to advance a different chemical series from a modestly potent HTS hit to the clinical-stage MTA-cooperative PRMT5 inhibitors TNG908 and TNG462
