In idiopathic pulmonary fibrosis, the lung tissue thickens and stiffens through proliferation of fibroblasts and invasion by inflammatory cells. One of the drivers of these processes is the enzyme autotaxin, which produces the signaling molecule lysophosphatidic acid. Several inhibitors of autotaxin have been reported, which show varying degrees of clinical potential.
Anti-inflammatory compounds can alleviate many acute and chronic diseases, including autoimmune, cardiovascular and neurodegenerative disorders. However, many such compounds increase risk of numerous adverse events because they inhibit not only cyclooxygenase-2 (COX-2), which induces pathological inflammation, but also COX-1, which is important for renal and gastrointestinal function.
The enzyme PARP1 helps repair single-stranded DNA breaks, and its inhibition shows antitumor efficacy in ovarian, breast, prostate and pancreatic cancers involving mutations in BRCA1 or BRCA2. However, resistance to PARP1 inhibition is a major problem.
Esophageal cancer is among the most lethal cancers with a high mortality rate worldwide. Chinese researchers have explored the potential link between long intergenic non-protein coding RNA 1354 (LINC01354) and esophageal cancer.
Myocardial ischemia-reperfusion (MI/R) injury is a major contributor to heart failure. The long noncoding RNA (lncRNA) myocardial infarction-associated transcript (MIAT) has been shown to worsen cardiac damage during ischemia, making it a promising target for RNA interference.
John Squires, the recently anointed director of the U.S. Patent and Trademark Office, has determined that a machine learning (ML) patent application met the standard for patent subject matter eligibility, an outcome that seems to bode well for ML-based patent applications going forward.
Merck KGaA has prepared and tested new antibody-drug conjugates (ADCs) comprising monoclonal antibodies targeting sodium-dependent phosphate transport protein 2B (SLC34A2; NaPi-2b) linked to exatecan through a β-glucuronidase cleavable linker. They are described as potentially useful for the treatment of ovarian and non-small-cell lung cancer.
Shanghai Apeiron Biotechnology Co. Ltd. has reported selenium-containing heterocyclic compounds acting as DNA polymerase theta (POLθ, POLQ) inhibitors potentially useful for the treatment of cancer.
AC Immune SA has synthesized thiazolo[5,4-c]pyridine-4(5H)-one derivatives acting as TAR DNA-binding protein 43 (TARDBP; TDP-43) aggregation ligands reported to be useful for the diagnosis of amyotrophic lateral sclerosis, Alzheimer’s disease, Parkinson’s disease, frontotemporal dementia, limbic-predominant age-related TDP-43 encephalopathy and traumatic encephalopathy.
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