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.
Jiangsu Hengrui Pharmaceuticals Co. Ltd. has patented new proteolysis targeting chimera (PROTACs) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to cyclin-dependent kinase 7 (CDK7) targeting moiety potentially useful for the treatment of cancer, inflammatory and autoimmune diseases.
Arvinas Inc. has identified new proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase coupled to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1)-targeting moiety acting as HPK1 degradation inducers designed for use in the treatment of cancer.
Hubei Bio-Pharmaceutical Industrial Technological Institute Inc. has identified new molecular glue degrader compounds acting as proto-oncogene Vav (VAV1)/protein cereblon (CRBN) interaction inducers for degradation of VAV1 reported to be useful for the treatment of inflammatory bowel disease.
Gluetacs Therapeutics (Shanghai) Co. Ltd. has discovered new proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN)-binding moiety coupled to a SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and SMARCA4-targeting moiety. They are designed for use in the treatment of cancer, transplant rejection, infections, diabetes, autoimmune, neurological, inflammatory and cardiovascular disorders, among others.
Retinoid X receptor γ (RXRγ) is a key nuclear receptor that sustains androgen receptor (AR) signaling. In castration-resistant prostate cancer (CRPC), RXRγ contributes to disease progression by maintaining adaptive transcriptional networks that promote therapy resistance and tumor cell survival.
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