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.
Boundless Bio Inc. has obtained IND approval from the FDA for its novel kinesin oral degrader program, BBI-940. A first-in-human trial (KOMODO-1) for metastatic breast cancer is expected to begin in the first half of this year.
Gan & Lee Pharmaceuticals Co. Ltd. has prepared and tested proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to an estrogen receptor α(ER-α; ESR1) targeting moiety via a linker reported to be useful for the treatment of cancer.
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