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.
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.
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