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.
Researchers from Flare Therapeutics Inc. presented the preclinical profile of FX-111, a selective active androgen receptor (ARON) degrader, in models of prostate cancer.
DNA methylation, catalyzed by DNMT enzymes, is a central epigenetic mechanism frequently disrupted in cancer, where aberrant hypermethylation contributes to tumor suppressor gene silencing. Researchers from Nankai University reported the discovery and preclinical characterization of [I], a selective DNMT1 degrader in models of acute myeloid leukemia (AML).
Beijing Innocare Pharma Tech Co. Ltd. has synthesized new antibody-drug conjugates comprising antibody or antigen-binding fragment covalently linked to eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1) degradation inducer potentially useful for the treatment of cancer.
Astrazeneca plc has exercised an option under its collaboration with Pinetree Therapeutics Inc. to obtain an exclusive global license to develop and commercialize PTX-299, a first-in-class bispecific antibody degrader targeting EGFR. The option exercise triggers a $25 million payment to Pinetree.
Gilead Sciences Inc. has identified new GTPase KRAS G12D mutant inhibitors and proteolysis targeting chimeras (PROTACS) comprising an E3 ubiquitin ligase-binding moiety covalently linked to a GTPase KRAS G12D mutant-targeting moiety potentially useful for the treatment of cancer.
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