For COVID-19, the limited durability of vaccines requires multiple injections, and their effectiveness is continuously challenged by emerging new spike variants of the virus. The SARS-CoV-2 main protease Mpro plays a role in major polyprotein processing events and is essential for viral replication.
Gut bacteria used liquid-liquid phase separation (LLPS) to organize themselves into condensates, which allowed them to adapt to nutrient deprivation, enabling them to colonize the gut. In experiments reported in the March 17, 2023, issue of Science, investigators showed that a mutant of the beneficial gut bacterium Bacteroides thetaiotaomicron was “highly defective in competitiveness, in its ability to colonize the mammalian gut,” senior author Eduardo Groisman told BioWorld. “Our paper provides the first example in which [LLPS] matters in bacterial host interactions.”
Impact Therapeutics (Shanghai) Inc. has divulged substituted tricyclic compounds acting as poly(ADP-ribose) polymerase (PARP; ARTD) inhibitors reported to be useful for the treatment of cancer.
Biofront Ltd. has described proteolysis targeting chimeras (PROTACs) comprising cereblon (CRBN) ligands coupled to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1) targeting moiety via linker acting as HPK1 degradation inducers reported to be useful for the treatment of cancer.
Jiangsu Hansoh Pharmaceutical Group Co. Ltd. and Shanghai Hansoh Biomedical Co. Ltd. have identified dual antagonists of endothelin ETA receptor and angiotensin AT1 receptor reported to be useful for the treatment of diabetes, hypertension and renal disorders.
Reistone Biopharma Co. Ltd. has synthesized quinolinofuran derivatives acting as MAP kinase-activated protein kinase 2 (MAPKAPK2; MK2) inhibitors reported to be useful for the treatment of fibrosis, autoimmune, inflammatory and metabolic disorders.
The neuron-specific K+/Cl- co-transporter KCC2 is involved in the shift from depolarizing to hyperpolarizing γ-aminobutyric acid receptor (GABAAR) currents and subsequent synaptic inhibition.
Investigators from the Thomas Jefferson University have presented a case report of a 27-year-old pregnant patient in whom cystic hygroma, extensive anasarca, bilateral pleural effusions, ascites, abnormally curved sacrum and hydrocephalus with parenchymal volume loss, among others were detected by prenatal imaging during pregnancy (onset was at about 21 weeks of gestation).
Acid sphingomyelinase deficiency (ASMD) is a progressive lysosomal storage disease caused by autosomal recessive pathogenic variants in the SMPD1 gene encoding acid sphingomyelinase (ASM). In a recent study, researchers from Albert Einstein College of Medicine aimed to assess the levels of plasma lyso-sphingomyelin, a deacylated form of sphingomyelin, in patients with ASMD pre- and post-treatment with olipudase alfa (recombinant-human acid sphingomyelinase).