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.
Scientists at Oncopia Therapeutics Inc. (dba SK Life Science Labs) and The University of Michigan have synthesized proteolysis targeting chimera (PROTAC) compounds comprising a cereblon E3 ubiquitin ligase-binding moiety coupled to a probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β)-targeting agent through a linker.
Kangbaida (Sichuan) Biotechnology Co. Ltd. has disclosed proteolysis targeting chimeras (PROTACs) comprising a cereblon (CRBN) ligand coupled to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1)-targeting moiety through a linker.
Work at Dark Blue Therapeutics Ltd. has led to the identification of proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety coupled to a MLLT1- or MLLT3-targeting moiety through a linker.
B-cell lymphoma 6 (BCL6) is an essential transcriptional factor for the humoral immune response. However, genomic deregulation of BCL6 contributes to the development of different types of lymphoma such as diffuse large B-cell lymphoma (DLBCL).
