Bristol Myers Squibb Co. (BMS) has disclosed new Ikaros family zinc finger protein 1 (IKZF1, Ikaros), IKZF2 (Helios), IKZF3 (Aiolos) and/or IKZF4 (Eos) degradation inducers potentially useful for the treatment of cancer.
Shanghai Meiyue Biotech Development Co. Ltd. has divulged molecular glue degraders comprising an E3 ubiquitin-protein ligase/proto-oncogene Vav (VAV1) interaction inducer and VAV1 degradation inducer. They are designed for potential use in the treatment of cancer, autoimmune diseases, cardiovascular, renal, metabolic, inflammatory and neurological disorders.
Neomorph Inc.’s NEO-811 is a molecular glue degrader designed to induce targeted degradation of ARNT and suppress this signaling pathway implicated in clear cell renal cell carcinoma (ccRCC). Targeting ARNT offers a complementary strategy to broadly disrupt oncogenic HIF signaling in ccRCC.
Researchers from Ruijin Hospital and Shanghai Jiao Tong University have patented molecular glue degraders, specifically eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1) degradation inducers that are potentially useful for the treatment of cancer, autoimmune disease and inflammatory disorders.
Tango Therapeutics Inc. has synthesized substituted piperidine-dione molecular glue degraders comprising E3 ubiquitin ligase-binding moiety and acting as HBS1-like protein (HBS1L; HBS1) degradation inducers for use in the treatment of cancer.
K2 Medicines (Nanjing) Co. Ltd. has identified new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety coupled to a cyclin-dependent kinase 4 (CDK4)- and/or CDK4/6 dual-targeting moiety. They are designed for use in the treatment of cancer, neurodegeneration, viral infection, cardiovascular and inflammatory disorders.
A Beone Medicines I GmbH and Beone Pharmaceutical (Suzhou) Co. Ltd. patent details new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety coupled to an interleukin-1 receptor-associated kinase 1 (IRAK-1)- and IRAK-4-targeting moiety. They are described as useful for the treatment of cancer, inflammatory disorders and autoimmune diseases.
Mixed lineage kinase domain-like pseudokinase (MLKL), a key effector of necroptosis, is highly expressed in hepatocellular carcinoma (HCC), and its targeting may promote parthanatos-mediated immunogenic cell death. Researchers from the Chinese Academy of Sciences and collaborators described the discovery and preclinical characterization of C-116, a MLKL PROTAC degrader developed using AI-assisted rational drug discovery.
Signal transducer and activator of transcription 3 (STAT3) is a central mediator of cytokine and growth factor signaling and is aberrantly activated in approximately 70% of human cancers. Persistent STAT3 signaling drives tumor proliferation, survival, metastasis, angiogenesis, immune evasion and inflammation. Researchers from the University of Michigan reported the discovery and preclinical characterization of SD-965, a selective STAT3 PROTAC degrader.
Accutar Biotechnology Inc. has synthesized new protein-protein interaction targeted chimera (PPI-TAC) compound comprising an E3 ubiquitin ligase-binding moiety covalently bound to a phosphatidylinositol 3-kinase α (PI3Kα)-targeting moiety. They act as PI3Kα H1047R mutant degradation inducers potentially useful for the treatment of cancer.
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