Details on the work leading to the discovery of the second-generation SARS-CoV-2 main protease (Mpro) inhibitor PF-7817883 (ibuzatrelvir) were disclosed recently by Pfizer Inc. The drug is in phase II clinical development for the treatment of adult individuals with COVID-19 symptoms who are not hospitalized.
The increasing resistance to intravenous artemisinin therapy for malaria highlights the urgent need for new treatments that offer better patient compliance and a single-dose cure to address this global health threat. Novartis AG recently presented the discovery, development and evaluation of aminoisoquinolines as fast-acting intravenous therapeutic agents for severe malaria treatment.
Researchers from Japan Tobacco Inc. presented the discovery and preclinical characterization of novel highly potent Keap1-Nrf2 protein-protein interaction (PPI) inhibitors.
It has been previously demonstrated that the activation of spleen tyrosine kinase (SYK) contributes to processes that are central to the pathogenesis of neurodegenerative diseases, such as Alzheimer’s disease (AD) and Parkinson’s disease (PD).
DNA polymerase θ (POLθ), repressed in somatic cells and overexpressed in several types of cancer, is crucial for DNA double-strand break repair during mitosis.
The TRPV6 calcium channel is overexpressed in several types of cancer deriving from epithelia where calcium control is unbalanced, such as prostate, colon or breast cancer, among others.
Essential branched-chain amino acids (BCAA) such as leucine, isoleucine or valine, cannot be synthesized by mammals, making them an obligate part of the diet.
Researchers from Astrazeneca plc presented the structure and preclinical characterization of a novel PCSK9 inhibitor, AZD-0780, being developed for the treatment of cardiovascular disease. A new potentially druggable functional binding pocket was identified on the PCSK9 C-terminal domain (CTD), and multiple fragment screens generated a single CTD-binding hit.
In obstructive sleep apnea (OSA), the collapse of the upper airway at sleep onset leads to a decrease in blood oxygen levels, frequent arousals from sleep and consequently fatigue and daytime sleepiness.
Researchers from Bristol Myers Squibb Co. disclosed the structure and presented preclinical data for the dual inhibitor of diacylglycerol kinases (DGK) α and ζ, BMS-986408. Optimization of a DGK-α-selective hit led to the synthesis of dual DGK-α and -ζ inhibitors.
