Researchers from Sichuan University and Chengdu Normal University have reported the discovery of novel G9a/GLP covalent inhibitors for the treatment of triple-negative breast cancer (TNBC).
PI3Kα H1047R accounts for one-third of all PI3Kα mutations and is associated with treatment resistance to targeted therapies in breast cancer treatment. In addition, treatment with selective PI3Kα inhibitors often results in significant adverse events such as hyperglycemia due to on-target toxicity.
Researchers from Bridgebio Pharma Inc. recently presented BBO-10203, a first-in-class, orally bioavailable, covalent small-molecule candidate designed to inhibit RAS-driven PI3Kα activity without affecting glucose metabolism.
Haisco Pharmaceutical Group Co. Ltd. has synthesized poly(ADP-ribose) polymerase 1 (PARP-1; ARTD1) inhibitors reported to be useful for the treatment of cancer.
Researchers from Blueprint Medicines Corp. presented data from a study that aimed to assess the effects of combining cyclin-dependent kinase 2 (CDK2) inhibitor BLU-222 with CDK4/6 inhibitors, such as palbociclib or ribociclib, to overcome CDK4/6 inhibitor resistance in HR-positive/HER2-negative breast cancer.
Synnovation Therapeutics Inc. has synthesized phosphatidylinositol 3-kinase α (PI3Kα) inhibitors reported to be useful for the treatment of cancer, congenital lipomatous overgrowth, vascular malformations, epidermal naevi and skeletal abnormalities and PIK3CA-related overgrowth spectrum (PROS).
Phosphoinositide 3-kinase (PI3K) is a key cell cycle pathway regulator involved in tumor growth and development. PI3Kα mutations in p110α subunit, H1047R and E542K/E545K are found in patients with several cancer types, including breast cancer and are targeted by approved drugs such as Piqray (alpelisib, Novartis AG).
Researchers from Insilico Medicine Inc. reported on ISM-5043, a novel KAT6A inhibitor aimed to be used for the treatment of refractory ER+ breast cancer.
Isozymes that are overexpressed in cancer and key in some metabolic processes are potential therapeutic targets. Previous studies found that phosphoenolpyruvate carboxykinase 2 (PCK2) is required by cancer cells for maintaining high metabolic activity and proliferation in some cancer types, but no small-molecule PCK2 inhibitors currently exist.
