Katalytic Therapeutics Inc. has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a phosphodiesterase PDE4-targeting moiety reported to be useful for the treatment of arthritis, Behçet’s disease, chronic obstructive pulmonary disease, non-small-cell lung cancer, inflammatory disorders, inflammatory bowel disease, psoriasis and rheumatoid arthritis.
Biotheryx Inc. has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a son of sevenless homolog 1 (SOS1) targeting moiety reported to be useful for the treatment of cancer.
The TNF receptor superfamily member herpesvirus entry mediator (HVEM or TNFRSF14), first identified as a receptor for viral infection, acts as a molecular switch, either activating or inhibiting the immune response depending on the interacting ligand. Previous work found that HVEM binding to B- and T-lymphocyte attenuator (BTLA) initiates an inhibitory signal to effector T cells and that targeting the HVEM-BTLA complex with an antibody reduced tumor growth in a humanized mouse model.
Lirum Therapeutics Inc. has presented data regarding their insulin-like growth factor receptor (IGF-1R) antagonist LX-101, which couples an IGF-1 variant to a cytotoxic methotrexate payload. The antitumoral activity of LX-101 was investigated in Ewing sarcoma and desmoplastic small round cell tumor.
Scientists at Jiangsu Hengrui Medicine Co. Ltd. and Shanghai Hengrui Pharmaceutical Co. Ltd. have synthesized protein arginine N-methyltransferase 5 (PRMT5) inhibitors reported to be useful for the treatment of cancer.
In a recently published study, researchers from Shandong Second Medical University and collaborators synthesized a new dual-gold(I) complex, named QB-1561, and tested its potential to inhibit drug-resistant cancer cells overexpressing ATP-binding cassette (ABC) transporters
Daewoong Pharmaceutical Co. Ltd. has described transcriptional coactivator YAP1/transcriptional enhancer factor (TEAD) interaction inhibitors reported to be useful for the treatment of cancer.
Using ALK+ lung cancer patient-derived cell lines, researchers have performed phosphoproteomic screening and identified guanylate kinase 1 (GUK1) as a TKI sensitive metabolic molecule in ALK-driven lung cancer.