Healzen Therapeutics Co. Ltd. has patented new proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1)-targeting moiety via a linker. They are reported to be useful for the treatment of cancer, hematological and autoimmune diseases.
Haisco Pharmaceutical Group Co. Ltd. has identified new proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase binding ligand coupled to probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α)-targeting agent through a linker acting as SMARCA2 degradation inducers and thus reported to be useful for the treatment of lung cancer.
Blueprint Medicines Corp. has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a cyclin dependent kinase 2 (CDK2)-targeting moiety through a linker reported to be useful for the treatment of cancer.
Astrazeneca AB has synthesized proteolysis targeting chimera (PROTAC) compounds comprising a protein cereblon (CRBN) binding moiety covalently linked to an estrogen receptor α (ER-α)-targeting moiety through a linker reported to be useful for the treatment of breast cancer.
Researchers at Shanghai Haiyan Pharmaceutical Technology Co. Ltd. and Yangtze River Pharmaceutical Group have disclosed proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase-binding moiety coupled to a polycomb protein EED-targeting moiety through linkers; they are reported to be useful for the treatment of cancer.
Researchers from the National Cancer Institute and their collaborators have presented data regarding a MLK3-degrading PROTAC, CEP1347-VHL-02, for treating triple-negative breast cancer.
B-cell lymphoma represents about 85% of non-Hodgkin lymphoma cases; therapeutic approaches are represented by Bruton tyrosine kinase (BTK) inhibitors, but still some issues, such as drug resistance and off-target toxicity, limit the clinical benefits.
Betta Pharmaceuticals Co. Ltd. has described proteolysis targeting chimera (PROTAC) compounds comprising a VHL-binding agent coupled to a GTPase KRAS-targeting moiety through a linker acting as KRAS degradation inducers reported to be useful for the treatment of cancer.