Tiger Biotherapeutics Inc. has disclosed proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase cereblon (CRBN)-binding moiety coupled to a GTPase KRAS (mutant)-binding moiety through a linker.
B-cell lymphoma 6 (BCL6) is up-regulated in several B-cell malignancies where it acts as a transcription factor activity mediator to induce and maintain lymphomagenesis.
Researchers at Rheinisch-Westfaelische Technische Hochschule Aachen University and University of Arizona have synthesized proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a DYRK1A and/or DYRK1B and/or DYRK2 and/or DYRK3 and/or CLK1 and/or CLK2 and/or CLK3 and/or CLK4 and/or HASPIN targeting moiety through a linker reported to be useful for the treatment of cancer, viral infection, diabetes, inflammatory disorders, Alzheimer’s, Parkinson’s, Huntington’s and autoimmune diseases, among others.
Curadev Pharma Ltd. has patented proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase coupled to mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1)-targeting agent via linker acting as HPK1 inhibitors and thus reported to be useful for the treatment of cancer, viral infections and immunological disorders.
Hangzhou Glubio Therapeutics Co. Ltd. has described proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase protein-binding moiety covalently linked to a Wee1-like protein kinase (Wee1)-binding moiety reported to be useful for the treatment of cancer.
Bristol Myers Squibb Co. has identified proteolysis targeting chimera (PROTAC) compounds comprising a E3 ubiquitin ligase-binding moiety coupled to a proto-oncogene tyrosine-protein kinase receptor Ret (RET; CDHF12; PTC) targeting moiety through a linker reported to be useful for the treatment of cancer.
Roivant Discovery Inc. has disclosed PROTACs (proteolysis targeting chimeras) comprising an E3 ubiquitin ligase binding moiety covalently linked to an E3 ubiquitin-protein ligase Mdm2 (Hdm2)-targeting moiety through a linker.
Scientists at the Institute of Cancer Research have generated a proteolysis targeting chimera (PROTAC) that successfully destroyed RIPK1 in cancer cells.
Shanghai- and San Diego-based Degron Therapeutics Inc. secured a potential $1.2 billion deal with Tokyo-headquartered Takeda Pharmaceutical Co. Ltd. May 23 for a multitarget collaboration and exclusive licensing agreement for molecular glue degraders. “It is a breakthrough technology in the small-molecule drug discovery field,” Degron CEO Lily Zou told BioWorld. “People talk about cell and gene therapy, but small molecules are still the mainstream of drug discovery, [with] more reach.”
Shanghai- and San Diego-based Degron Therapeutics Inc. secured a potential $1.2 billion deal with Tokyo-headquartered Takeda Pharmaceutical Co. Ltd. May 23 for a multitarget collaboration and exclusive licensing agreement for molecular glue degraders. “It is a breakthrough technology in the small-molecule drug discovery field,” Degron CEO Lily Zou told BioWorld. “People talk about cell and gene therapy, but small molecules are still the mainstream of drug discovery, [with] more reach.”
