Innocure Therapeutics Inc. has divulged piperidinediones as proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase cereblon (CRBN)-binding moiety covalently linked to bromodomain-containing protein 4 (BRD4)- and/or tyrosine-protein phosphatase non-receptor type 11 (PTPN11)-targeting moiety via linker reported to be useful for the treatment of cancer.
Halda Therapeutics Opco Inc. has patented proteolysis-targeting chimeric (PROTAC) compounds comprising an E3 ubiquitin ligase cereblon (CRBN)-binding moiety covalently bonded to a protein-targeting moiety via linker reported to be useful for the treatment of cancer and hepatitis.
Kymera Therapeutics Inc. has divulged proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN)-binding moiety covalently linked to interleukin-1 receptor-associated kinase 4 (IRAK-4)-targeting moiety reported to be useful for the treatment of cancer.
Biogen Inc. and C4 Therapeutics Inc. have disclosed proteolysis targeting chimera (PROTAC) compounds comprising a degradation signaling moiety such as E3 ubiquitin ligase-binding moiety covalently linked to a Bruton tyrosine kinase (BTK)-targeting moiety through a linker reported to be useful for the treatment of leukemia and lymphoma, multiple sclerosis, atopic dermatitis, rheumatoid arthritis and systemic lupus erythematosus.
Chengdu Easton Biopharmaceuticals Co. Ltd. has described proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) ligand binding moiety covalently bound to a bromodomain-containing protein 4 (BRD4; HUNK1)-targeting moiety through a linker.
Sichuan Haisco Pharmaceutical Co. Ltd. has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently bonded to an EGFR (HER1; erbB1) targeting moiety through a linker reported to be useful for the treatment of non-small-cell lung cancer (NSCLC).
Jiangsu Hengrui Medicine Co. Ltd. and Shanghai Hengrui Pharmaceutical Co. Ltd. have patented proteolysis targeting chimera (PROTAC) compounds comprising E3 ubiquitin ligase-binding moiety covalently bonded to estrogen receptor-α (ERα)-targeting moiety through a linker reported to be useful for the treatment of breast cancer and infections.
Kirsten rat sarcoma viral oncogene (KRAS) is one of the GTPases from the RAS family activating signaling pathways that regulate cell functions. KRAS mutation of glycine to aspartate at position 12 (G12D) is a common mutation in pancreatic ductal adenocarcinoma, colorectal cancer, lung adenocarcinoma and other solid tumors. ASP-3082 is a proteolysis targeting chimera (PROTAC) under development by Astellas Pharma Inc. The company has presented the first in vitro and in vivo results of this new compound.
