Biopolar Hongye (Nantong) Pharmaceutical Co., Ltd. has described proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase cereblon (CRBN) binding moiety covalently linked to a Bruton’s tyrosine kinase (BTK) binding moiety reported to be useful for the treatment of cancer, inflammatory and autoimmune diseases.
Several recent Celgene Corp. patents detail the development of proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN)-binding moiety covalently linked to an interleukin-1 receptor-associated kinase 4 (IRAK-4)-targeting moiety via a linker.
Foghorn Therapeutics Inc. has disclosed proteolysis targeting chimera (PROTAC) compounds comprising ubiquitin ligase binding moieties covalently linked to a probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and/or transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) targeting moiety reported to be useful for the treatment of cancer and viral infection.
TYK Medicines Inc. has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently bonded to an EGFR (mutant)-targeting moiety through a linker.
Nimbus Saturn Inc. has identified proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase-binding moiety covalently linked to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1)-targeting moiety linked via a linker.
Work at Foghorn Therapeutics Inc. has led to the design of proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding agent coupled to CREB-binding protein (CREBBP; CBP)-targeting moiety through a linker acting as CBP degradation inducers.
Data from preclinical studies conducted to evaluate the activity of NKT-3964, a first-in-class, orally bioavailable CDK2-selective PROTAC degrader being developed for the potential treatment of cancer, were reported by Nikang Therapeutics Inc.
Shanghai Huilun Pharmaceutical Co. Ltd. has synthesized proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin-protein ligase binding moiety coupled to an interleukin-1 receptor-associated kinase 4 (IRAK-4) targeting moiety through a linker reported to be useful for the treatment of cancer, neurodegeneration, infections, autoimmune disorders, metabolic diseases, cardiovascular disorders, genetic diseases and inflammatory disorders, among others.
Nanjing Mingde New Drug Research Co. Ltd. has designed proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a GTPase KRAS (G12D mutant)-targeting moiety via a linker for the treatment of cancer.
