Triple-negative breast cancer (TNBC) cells depend on the transcriptional kinases CDK12 and CDK13 to maintain DNA damage response gene expression and manage replication stress. Due to their functional overlap, inhibition of a single kinase may permit compensatory activity.
Beijing Innocare Pharma Tech Co. Ltd. has gained IND clearance in China to conduct clinical trials of ICP-538, an orally administered molecular glue degrader targeting VAV1, which is a key protein downstream of T-cell and B-cell receptors. ICP-538 is being studied for the treatment of autoimmune diseases, such as inflammatory bowel disease, systemic lupus erythematosus and multiple sclerosis.
Uppthera Inc. has patented new proteolysis targeting chimera (PROTAC) compounds comprising cereblon E3 ubiquitin ligase-binding moiety covalently linked to Aurora kinase A (AURKA; ARK1)-targeting moiety. They are reported to be useful for the treatment of cancer.
Inflammatory bowel disease (IBD), including ulcerative colitis and Crohn’s disease, is a chronic immune-mediated inflammatory disorder with limited long-term therapeutic options. Proteolysis-targeting chimeras (PROTACs) offer a promising strategy for IBD by enabling selective degradation of disease-relevant proteins and potentially improving efficacy and safety.
Kazia Therapeutics Ltd. has announced promising preclinical and translational data supporting the development of NDL-2, a protein degrader targeting a newly identified mechanism of immunotherapy resistance and metastatic progression.
Shanghai Haiyan Pharmaceutical Technology Co. Ltd. and Yangtze River Pharmaceutical Group have divulged new isoindoline proteolysis targeting chimeric (PROTAC) compounds comprising cereblon (CRBN) ligands covalently linked to a eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1)-targeting moiety. They are reported to be useful for the treatment of cancer.
Chia Tai Tianqing Pharmaceutical Group Co. Ltd. has disclosed proteolysis targeting chimeric (PROTAC) compounds comprising a E3 ubiquitin ligase-binding moiety covalently linked to an estrogen receptor-α (ERα)-targeting moiety. They are reported to be useful for the treatment of breast cancer.
Ovarian cancer is a highly lethal gynecological malignancy with limited therapeutic options for recurrent and drug-resistant disease. Sirtuin 2 (SIRT2) promotes tumor cell proliferation, migration and invasion by regulating multiple oncogenic signaling pathways. Although SIRT2 has emerged as a promising therapeutic target, conventional inhibitors often result in incomplete and transient suppression of its activity.
Gachon University and Jeonbuk National University Industry Foundation have disclosed proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety coupled to a serine/threonine-protein kinase PAK4-targeting moiety through a linker potentially useful for the treatment of cancer.
Hanmi Holdings Co. Ltd. has patented proteolysis targeting chimeras (PROTACs) comprising a cereblon (CRBN)-binding moiety coupled to a histone acetyltransferase p300 (EP300)-targeting moiety through a linker acting as EP300 degradation inducers reported to be useful for the treatment of cancer.
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