Experimental drugs that directly inhibit the NSD2 enzyme have shown potential as an effective strategy against hard-to-treat cancers, such as lung and pancreatic tumors driven by KRAS mutations. The therapeutic mechanism involves reversing a histone H3 methylation that promotes open chromatin and the expression of oncogenes. Read More
Telomir Pharmaceuticals Inc. has released new in vitro data revealing that Telomir-1 potently inhibits three key histone demethylase enzymes – JMJD3, FBXL10 and FBXL11 – that regulate gene expression through epigenetic mechanisms. Read More
Phosphorylation of the protein Tau is a key post-translational feature in tauopathies like Alzheimer’s disease (AD), which leads to microtubule dysfunction and Tau accumulation. Recent findings have suggested the blockade of the adenosine A2A receptor as an approach that improves the outcome in amyloid and Tau models. Read More
Seed Therapeutics Inc. has gained IND clearance from the U.S. FDA for ST-01156, a brain-penetrant RBM39 degrader. The clearance enables initiation of a first-in-human phase I trial in patients with advanced solid tumors and hematological malignancies, prioritizing biomarker-selected RBM39-dependent cancers. Dosing is expected to begin in the first quarter of next year. Read More
Open Source Therapeutics Co. Ltd. has identified bifunctional epoxide hydrolase 2 (EPHX2; sEH) inhibitors reported to be useful for the treatment of chronic obstructive pulmonary disease (COPD), Alzheimer’s disease, epilepsy, hypertension, psoriasis, rheumatoid arthritis, stroke and ulcerative colitis, among others. Read More
Melanoma is one of the most mutation-prone cancers, with 90% of cases involving the V600E mutation in BRAF kinase. Several therapies are available against melanoma, but each one is associated with substantial drawbacks. Researchers at Shanghai Institute of Materia Medica of the Chinese Academy of Sciences and collaborators reasoned that it might be effective to simultaneously inhibit both angiogenesis and immunosuppression in the tumor microenvironment. Read More
Scenic Biotech BV has synthesized lysosomal phospholipase A and acyltransferase (PLA2G15) inhibitors reported to be useful for the treatment of HIV infection, frontotemporal dementia, Niemann-Pick disease type C, Batten disease, Alzheimer’s disease and Parkinson’s disease. Read More
Chengdu Chipscreen Pharmaceutical Ltd. has divulged Werner syndrome ATP-dependent helicase (WRN; RECQ3; RECQL2) inhibitors reported to be useful for the treatment of cancer. Read More
Chronic infection with the parasitic protozoan Cryptosporidium can cause debilitating diarrhea and lead to cognitive impairment and cachexia. Researchers at the University of Washington and collaborators have identified the 5-aminopyrazole-4-carboxamide BKI-1708 as an inhibitor of calcium-dependent protein kinase 1, which is highly expressed during proliferation of the parasite. Read More
Temple University has described compounds acting as antioxidants and nuclear factor erythroid 2-related factor 2 (NFE2L2; NRF2) activators reported to be useful for the treatment of Alzheimer’s disease, Parkinson’s disease, Huntington’s disease, cerebral palsy, epilepsy and multiple sclerosis. Read More
Overexpression of the eukaryotic translation initiation factor 4E (eIF4E) has been observed in a wide range of tumors, where it is associated with malignant transformation, tumor progression, poor prognosis, and resistance to therapy. Read More
