Ningbo Newbay Medical Technology Co. Ltd. has identified helicase bicycle amide derivatives acting as DNA polymerase θ (POLθ, POLQ) inhibitors 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.
Researchers from Sagittide Therapeutics Co. Ltd. and Shanghai Jiao Tong University have presented results of early studies with a novel MUC1-C-targeted near-infrared imaging agent – SAG-602 – for fluorescence-guided surgery of cancer.
MYC is a key regulator of RNA Polymerase I (Pol I) transcription, promoting rRNA synthesis both directly and indirectly. MYC overexpression is common in many cancer types, where it drives increased ribosome biogenesis to support uncontrolled cell growth and proliferation.
Aprea Therapeutics Inc. has announced new preclinical data on APR-1051, the company’s next-generation oral WEE1 inhibitor, in human papillomavirus (HPV)-positive head and neck squamous cell carcinoma (HNSCC).
Haisco Pharmaceutical Group Co. Ltd. has identified new proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase binding ligand coupled to probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α)-targeting agent through a linker acting as SMARCA2 degradation inducers and thus reported to be useful for the treatment of lung cancer.
Diffuse midline gliomas (DMGs) are pediatric brain tumors with a very dismal prognosis since less than 5% of patients survive 2 years after diagnosis. Radiotherapy remains the standard treatment for DMG, and several combination chemotherapies and single-agent target therapies are currently being explored.
MYB is an oncogenic transcription factor that is often aberrantly expressed in hematologic malignancies, mostly in acute myeloid leukemia (AML). Rgenta Therapeutics Inc. recently presented data for RGT-61159, a potent and selective MYB inhibitor compound that demonstrated cell killing across a panel of MYB-overexpressing leukemic cell lines.
Glioblastoma is the most frequent and aggressive primary brain cancer in adults, and patients can expect to live shorter than 2 years, regardless of therapy. The cancer can be treated with CAR T cells, but many patients develop resistance because tumors mutate or delete the antigens recognized by the T cells, while the tumor microenvironment suppresses T-cell activity.
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