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.
Glutathione S-transferase (GSTP) is an enzyme involved in the detoxification of several xenobiotics such as tobacco carcinogens or cisplatin drugs and is overexpressed in KRAS-mutant lung, colon and pancreatic cancer, among others. The upregulation of GSTP may partially contribute to chemotherapy and radiotherapy resistance.
Poly (ADP-ribose) polymerase (PARP) inhibitors are used as maintenance therapy after completion of platinum-based chemotherapy in ovarian cancer. However, acquired or de novo resistance to PARP inhibitors is frequent and limits their application.
Researchers from Novacyte Therapeutics Co. Ltd. presented preclinical data for NC-18, a novel HER2-targeting antibody drug conjugate (ADC) being developed for the treatment of HER2-positive/expressing advanced solid tumors.
Cyclins and cyclin-dependent kinases (CDKs) regulate the activity of E2F and Rb to drive cell cycle progression. Disrupting this interaction has shown lethality in cancer cells harboring alterations that lead to higher expression of E2F1.
Claudin 18.2 (CLDN18.2) is a member of the claudin family and is overexpressed in gastric, gastroesophageal junction and pancreatic cancer, among others. Researchers from Elevation Oncology Inc. recently presented preclinical efficacy data on the combination of EO-3021, an antibody-drug conjugate (ADC) targeting CLDN18.2, with VEGFR-2 or PD-1 inhibitors in models of gastric adenocarcinoma.
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