Hangzhou Zhongmei Huadong Pharmaceutical Co. Ltd. has synthesized proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently bonded to a GTPase KRAS (G12D mutant) targeting moiety through a linker reported to be useful for the treatment of cancer.
Hangzhou Zhongmei Huadong Pharmaceutical Co. Ltd. has described proteolysis targeting chimera (PROTACs) 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. They are reported to be useful for the treatment of cancer.
Captor Therapeutics Inc. has disclosed proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase-binding moiety covalently linked to an induced myeloid leukemia cell differentiation protein MCL-1-targeting moiety through a linker.
Uppthera Inc. has described proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety coupled to a serine/threonine-protein kinase PLK1 (STPK13) targeting moiety through a linker. They are reported to be useful for the treatment of cancer and neurological disorders.
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.
