In tumoral cells, the modulation of the G1/S phases of cell cycle is destabilized by amplification and high expression of cyclin E (CCNE) or by mutation or loss of retinoblastoma 1 (RB1) gene. Cancer cells meeting these characteristics have been sown to be highly sensitive to cyclin-dependent kinase 2 (CDK2) depletion.
Ideaya Biosciences Inc. has nominated IDE-251, a dual KAT6/7 inhibitor targeting 8p11 amplification tumors in breast and lung cancers, as a development candidate. IDE-251 is an equipotent, highly selective, small-molecule dual inhibitor of KAT6 and -7, both of which have been shown to support cancer cell survival.
Endocrine therapy against the estrogen receptor (ER) is widely used for the treatment of ER+ breast cancer. Selective estrogen receptor degraders (SERDs) compete directly with estrogen for ER binding and create an unstable protein complex that leads to proteasome-mediated ER protein degradation.
China’s National Medical Products Administration (NMPA) granted new approvals to several Chinese biopharmaceuticals this week, including expanding indications of four different cancer drugs and clearing one sublingual tablet for stroke.
Scientists at Beigene Ltd. and Beigene Switzerland GmbH have identified phosphatidylinositol 3-kinase α (PI3Kα) (H1047R mutant) 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).
