Arvinas Inc. has identified new proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase coupled to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1)-targeting moiety acting as HPK1 degradation inducers designed for use in the treatment of cancer.
Biofront Ltd. has designed new proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase-binding moiety coupled to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1)-targeting moiety as HPK1 degradation inducers. They are described as potentially useful for the treatment of cancer.
Mitogen-activated protein kinase kinase kinase kinase 1 (HPK1) is a serine/threonine protein kinase that is expressed in the hematopoietic compartment, exerting regulatory functions in myeloid and innate immune cells. It has been associated with decreased T-cell activation and proliferation.
Merck KGaA has synthesized proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin-protein ligase-binding moiety covalently bonded to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1)-targeting moiety through a linker reported to be useful for the treatment of cancer.
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.
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.
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.
Biofront Ltd. has described proteolysis targeting chimeras (PROTACs) comprising cereblon (CRBN) ligands coupled to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1) targeting moiety via linker acting as HPK1 degradation inducers reported to be useful for the treatment of cancer.
