Recent Highlights in Targeted Protein Degradation

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  • Опубліковано 1 сер 2024
  • 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.
    Sign up for future sessions here: lu.ma/w1q906iz
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