LG Chem Ltd. has disclosed bromodomain-containing protein 4 (BD1 domain) (BRD4 BD1) and CREB-binding protein (CREBBP; CBP) inhibitors reported to be useful for the treatment of cancer, inflammatory disorders and autoimmune disease.
Lung cancer, which often occurs as lung adenocarcinoma, is the leading cause of cancer-related death worldwide. At least 70% of lung adenocarcinoma patients fail to show long-term benefit from immune checkpoint inhibitors, highlighting the need to identify in advance those more likely to benefit.
Researchers continue to search for how they can inhibit cancer metastasis as it can severely worsen prognosis, even if the primary tumor responded well to therapy. Researchers at Università degli Studi di Torino and collaborators previously showed that injecting an RNA aptamer targeting the miRNA miR-214, called anti-miR-214 sponge, reduced metastasis of tumors to lungs and liver. One drawback of this potential therapeutic approach was that the inhibitor oligo could enter all cells, not only tumors.
Triple-negative breast cancer (TNBC) accounts for a substantial proportion of all breast cancers and is the most aggressive form of the disease. Identifying potential therapeutic targets is critical because the cancer does not express the three surface receptors recognized by current targeted therapies.
Chengdu Chipscreen Pharmaceutical Ltd. has divulged Werner syndrome ATP-dependent helicase (WRN; RECQ3; RECQL2) inhibitors reported to be useful for the treatment of cancer.
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.
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.
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.
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.
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