Genescience Pharmaceutical Co. Ltd. has presented data on a new STAT6 PROTAC degrader – GenSciP166 – which selectively targets STAT6 for proteasomal degradation. GenSciP166 was assayed in vitro as well as in vivo in the MC903 atopic dermatitis murine model.
Prelude Therapeutics Inc. has identified new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase Von Hippel-Lindau disease tumor suppressor (VHL)-binding moiety coupled to a probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α)- and SMARCA4-targeting moiety.
Work at Blueprint Medicines Corp. to identify a selective and potent CDK4 degrader led to the identification of BLU-448, with minimal activity against CDK6 for treating HR+/HER2- breast cancer.
Foghorn Therapeutics Inc. has synthesized proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding agent coupled to a histone acetyltransferase p300 (EP300)-targeting moiety. As such, they are described as EP300 degradation inducers potentially useful for the treatment of cancer.
The University of California has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase Von Hippel-Lindau disease tumor suppressor (VHL)-binding moiety coupled to cAMP-dependent protein kinase catalytic subunit α (PRKACA) targeting moiety through a linker.
SMARCA4-deficient cells have shown dependency on SMARCA2 for survival, suggesting SMARCA2 as a promising synthetic lethal target in SMARCA4-deficient cancers. Chinese researchers recently published data on a series of SMARCA2 PROTACs, among which compound [I] exerted good SMARCA2 degradation.
At the recently concluded Digestive Disease Week, researchers from Kymera Therapeutics Inc. presented preclinical efficacy data on KT-579, a selective oral IRF5 degrader, in models of IBD.
Genosco Inc. has patented new molecular glue degraders comprising cereblon-binding agents acting as GSPT and/or Myc proto-oncogene protein (c-Myc) degradation inducers designed for use in the treatment of cancer.
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