Aurigene Discovery Technologies Ltd. has divulged fused isoxazolyl compounds acting as histone acetyltransferase KAT6A (monocytic leukemia zinc finger protein; MOZ; MYST-3) inhibitors reported to be useful for the treatment of cancer.
Biogen Inc. and C4 Therapeutics Inc. have disclosed proteolysis targeting chimera (PROTAC) compounds comprising a degradation signaling moiety such as E3 ubiquitin ligase-binding moiety covalently linked to a Bruton tyrosine kinase (BTK)-targeting moiety through a linker reported to be useful for the treatment of leukemia and lymphoma, multiple sclerosis, atopic dermatitis, rheumatoid arthritis and systemic lupus erythematosus.
Does cancer cause autoimmune disease or is it the other way around? In looking at the question of which comes first, the chicken or the egg, researchers at the Garvan Institute of Medical Research in Australia found that a genetic mutation that alters immune cells in leukemia is behind certain autoimmune disorders.
Chengdu Easton Biopharmaceuticals Co. Ltd. has described proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) ligand binding moiety covalently bound to a bromodomain-containing protein 4 (BRD4; HUNK1)-targeting moiety through a linker.
Parenchyma Biotech Inc. has described aryl hydrocarbon receptor (AhR) agonists reported to be useful for the treatment of cancer and autoimmune disease.
HKSH Medical Group (HKSH) has adopted droplet digital polymerase chain reaction (ddPCR) for minimal residual disease (MRD) monitoring to track the status of patients with leukemia.
Targeting tyrosine-protein kinase Lck (LCK) with dasatinib has demonstrated activity against T-cell acute lymphoblastic leukemia (T-ALL). To make the effects more lasting, researchers from St. Jude Children's Research Hospital and the University of Pennsylvania designed proteolysis targeting chimeras (PROTACs) using dasatinib as an LCK ligand and phenyl-glutarimide as a cereblon-directing moiety.
University of Michigan has described new proteolysis targeting chimeric (PROTACs) compounds comprising cereblon (CRBN) ligands covalently bonded to CREB-binding protein (CBP) and/or histone acetyltransferase KAT3B (p300)-targeting moiety through linker reported to be useful for the treatment of cancer.
Arginases play key roles in metabolic pathways. Arginase 1 (ARG1) is expressed by myeloid cells in the tumor microenvironment and suppresses the functioning of T and NK cells.
A patient’s death has prompted the FDA to place a partial clinical hold on Curis Inc.’s phase I/IIa study of emavusertib in leukemia. The patient, who had relapsed or refractory acute myeloid leukemia, experienced several conditions. One of them was rhabdomyolysis, a dose-limiting toxicity of emavusertib. Rhabdomyolysis is a breakdown of muscle fibers in the blood.
