Merck KGaA has synthesized proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin-protein ligase-binding moiety covalently bonded to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1)-targeting moiety through a linker reported to be useful for the treatment of cancer.
Les Laboratories Servier SAS and Vernalis (R&D) Ltd. have disclosed son of sevenless homolog 1 (SOS1) inhibitors reported to be useful for the treatment of cancer, immunological and genetic disorders.
Spica Therapeutics NV has been awarded a 2-year €1.0 million (US$1.2 million) grant from Flanders Innovation & Entrepreneurship (VLAIO) to accelerate the development of the company’s lead anti-CD163 depleting monoclonal antibody program in oncology, advancing it toward early IND-enabling studies.
Foresight Therapeutics (Hefei) Co. Ltd. has described Werner syndrome ATP-dependent helicase (WRN; RECQ3; RECQL2) inhibitors reported to be useful for the treatment of cancer.
Genescience Pharmaceuticals Co. Ltd. has identified camptothecin derivatives acting as DNA topoisomerase I inhibitors reported to be useful for the treatment of cancer.
Chia Tai Tianqing Pharmaceutical Group Co. Ltd. has synthesized proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1) targeting moiety via a linker reported to be useful for the treatment of cancer.
Ensem Therapeutics Inc. has disclosed phosphatidylinositol 3-kinase α (PI3Kα) inhibitors, particularly PI3Kα mutant inhibitors, reported to be useful for the treatment of cancer.
Hypoxia is a common event in the microenvironment of solid tumors, triggering some changes in gene expression profiles to adapt to low-oxygen levels. Increasing evidence exists regarding hypoxia and mitochondrial dysfunction to play a role in the progression of non-small-cell lung cancer (NSCLC).
It is known that phosphatidylinositol 5-phosphate 4-kinase, type II, γ (PIP4K2C) is a lipid kinase tied to poor outcomes in a variety of cancers, such as colorectal (CRC) and breast cancers. In the search for PIP4K2C degraders, researchers from Larkspur Biosciences Inc. discovered LRK-4189, a cereblon-mediated PIP4K2C degrader.
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