Hinova Pharmaceuticals Inc. has divulged proteolysis targeting chimeric (PROTAC) compounds comprising a protein cereblon (CRBN) binding moiety covalently bound to an estrogen receptor (ER)-targeting moiety through a linker.

Researchers from Third Military Medical University of the Chinese PLA have published data from a study that aimed to investigate the biological functions and molecular mechanisms of tandem C2 domains, nuclear (TC2N) in the development and progression of breast cancer.

Synnovation Therapeutics Inc. has identified phosphatidylinositol 3-kinase α (PI3Kα) inhibitors reported to be useful for the treatment of cancer, PIK3CA-related overgrowth spectrum (PROS), congenital lipomatous overgrowth, vascular malformations, epidermal naevi and skeletal abnormalities.

Onkure Inc. has received FDA clearance of its IND application for OKI-219, a mutant selective PI3Kα H1047R inhibitor, for solid tumors.

Retinoic acid receptor-γ (RARγ) agonism is a key factor in CD8 T-cell-mediated immunity to infectious pathogens. The lack of studies on the effects of RARγ agonists on in vivo tumor growth of triple-negative (TNBC) or HER2+ breast cancers make it necessary to investigate whether RARγ could play a critical role in T-cell-mediated immunity in these breast cancers, using novel RARγ nuclear agonists.

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.