China Resources Pharmaceutical Research Institute (Shenzhen) Co. Ltd. has synthesized tricyclic heterocyclic compounds acting as protein arginine N-methyltransferase 5 (PRMT5) inhibitors reported to be useful for the treatment of cancer.
Iambic Therapeutics Inc. presented preclinical data on IAM-1363, a selective and irreversible HER2 and pan-HER2 mutant inhibitor in HER2-driven NSCLC models. In vitro studies across a panel of HER2-altered NSCLC cell lines demonstrated that IAM-1363 exhibits potent antiproliferative activity in both HER2-amplified and HER2-mutant models.
Methylenetetrahydrofolate dehydrogenase 2 (MTHFD2), an enzyme involved in one-carbon metabolism, is significantly overexpressed in cancer cells but shows limited expression in normal tissues, making it a promising target for cancer therapy.
Boehringer Ingelheim Pharma GmbH & Co. KG has disclosed glutaminyl-peptide cyclotransferase (QPCT; QC) and glutaminyl-peptide cyclotransferase-like protein (QPCTL; IsoQC) inhibitors reported to be useful for the treatment of cancer, fibrosis, atherosclerosis and more.
Summit Therapeutics Inc.’s presentation for bispecific antibody ivonescimab in non-small-cell lung cancer could draw some extra attention at next month’s World Conference on Lung Cancer meeting thanks to promising overall survival data from partner Akeso Pharmaceuticals Inc.’s China study of the PD-1/VEGF candidate.
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).
Small-cell lung cancer (SCLC) and some other cancers involve dysregulation of the transcription factor E2F, and apoptosis can be induced in those cells by blocking the interaction of the RxL sequence motif in E2F with cyclin A, which leads to hyperactivation of E2F. Researchers from Dana-Farber Cancer Institute and collaborators have developed macrocyclic peptides that inhibit this interaction and thereby hyperactivate E2F, leading to anticancer activity in various preclinical systems.
Despite having lower smoking habits than other groups in the U.S., Black Americans are more likely to develop lung cancer, and their survival rates are significantly worse. What explains this disparity? Scientists at Vanderbilt University Medical Center have analyzed the genetics of their African ancestry in search of risk genes related to the disease and tobacco use. The results reveal new risk factors and confirm the presence of genetic variants that may contribute to the greater impact of lung cancer in this population.