Zhuhai Yufan Biotechnologies Co. Ltd. has identified molecular glue degraders comprising an E3 ubiquitin protein ligase-binding agent covalently bound to a DNA-binding protein Ikaros (IKZF1)-targeting moiety acting as IKZF1 degradation inducers potentially useful for the treatment of cancer, autoimmune disease, neurodegeneration and inflammatory disorders.
VAV1 is a guanine nucleotide exchange factor essential for T- and B-cell receptor signaling, with expression largely restricted to immune cells. Loss of VAV1, via CRISPR or genetic deletion, impairs effector functions in both T and B cells.
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.
RSS
