We analyzed the precise ligand:receptor interactions required for activation of the muscarinic acetylcholine receptor M, a prototypical G protein-coupled receptor and potential diabetes target. Starting from literature-known compounds and docking solutions, ligands were tailored for the modulation of this receptor's activation. Several aspects of the structure-activity relationship of agonists were investigated in atomistic detail, in order to delineate how the receptor can be activated via the orthosteric site.
View Article and Find Full Text PDFJ Pharmacol Exp Ther
August 2021
Ferroptosis is a form of oxidative cell death that is increasingly recognized as a key mechanism not only in neurodegeneration but also in regulated cell death, causing disease in other tissues. In neurons, major hallmarks of ferroptosis involve the accumulation of lipid reactive oxygen species (ROS) and impairment of mitochondrial morphology and function. Compounds that interfere with ferroptosis could provide novel treatment options for neurodegenerative disorders and other diseases involving ferroptosis.
View Article and Find Full Text PDFRNase P is an essential enzyme responsible for tRNA 5'-end maturation. In most bacteria, the enzyme is a ribonucleoprotein consisting of a catalytic RNA subunit and a small protein cofactor termed RnpA. Several studies have reported small-molecule inhibitors directed against bacterial RNase P that were identified by high-throughput screenings.
View Article and Find Full Text PDFThe anterior nares are the main ecological niche for , an important commensal and opportunistic pathogen. Medical students are frequently colonized by a variety of pathogens. Microbial interactions in the human nose can prevent or favor colonization by pathogens, and individuals colonized by pathogens have increased risk of infection and are the source of transmission to other community members or susceptible individuals.
View Article and Find Full Text PDFThis study determines the development rates of the immature stages of the fly Ophyra albuquerquei Lopes, 1985. In this study, with 70% relative humidity and a 12-h photophase, eggs, larvae, and pupae were kept in a biochemical oxygen demand chamber at temperatures of 10, 15, 17, 20, 22, 25, 27, 30, 33, 35, and 40°C. While the rearing temperature increases, the development time for each immature stage of O.
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