In this Drug Hunter Flash Talk, we discuss scientific highlights from small molecules that induce the degradation of their targets of interest, with a focus on molecules that have recently demonstrated important proofs-of-concept in the clinic.
The talk covers:
-Theoretical advantages of targeted protein degradation over traditional small molecules
-Recent highlights throughout the industry illustrating these advantages
-Areas to watch in targeted protein degradation on the horizon
-Some of the highlights mentioned in the talk include:
-9:00: Ten ways degraders can differentiate in theory
-14:47: Agnostic to ligand mode of action: AR degraders
-16:18: AR degraders and ER degraders from Arvinas (bavdegalutamide/ARV-110, ARV-766, and ARV-471)
-18:58: MDM2 degraders from Kymera (e.g. KT-253)
-20:30: BRAF and allosteric EGFR degraders from C4 and Roche (e.g. CFT1946, CFT8919)
-21:43: IRAK4 degraders from Kymera (e.g. KT-474)
-22:54: BRD9 and BRM/BRG1 degraders from C4 Therapeutics and Prelude Therapeutics
-24:41: BTK degraders from Nurix (e.g. NX-2127, NX-5948)
-26:24: IV STAT3 degraders from Kymera Therapeutics (e.g. KT-333 and KT-003)
-27:45: RIPK2 degraders from GSK and PCSK9 degraders from Merck
-28:55: EGFR L858R degrader from Roche and C4 (e.g. compound 144)
-30:32: PCSK9 degrader from Merck (e.g. compound 16)
-32:17: A tissue-selective Bcl-XL degrader from Dialectic Therapeutics (e.g. DT2216)
-33:31: BRAF degrader from C4 Therapeutics (e.g. CFT1946)
-35:00: Brain-penetrant degraders
-36:20: A cyclin D1 degrader from Mt. Sinai (e.g. MS28)
- 37:38:Ten ways degraders can differentiate in theory
-38:22: Areas to watch in targeted protein degradation on the horizon:
Presented by: Dennis Hu, CEO & Editor-in-Chief, Drug Hunter with co-host Pierre Morieux, Chemistry Product Marketing Manager, Revvity Signals.
Presented on June 28, 2023, as part of the Drug Hunter Flash Talk series.
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