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Low-molecular-weight Ligand of the Thyroid-stimulating Hormone Receptor with the Activity of a Partial Agonist and a Negative Allosteric Modulator.
Dokl Biochem Biophys
January 2025
I.M. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St. Petersburg, Russia.
Graves' disease is caused by overactivation of the thyroid-stimulating hormone receptor (TSHR). One approach for its treatment may be the use of negative allosteric modulators (NAM) of TSHR, which normalize TSHR activity and do not cause thyroid hormone (TH) deficiency. The aim of the work was to study the effect of a new compound 5-amino-4-(4-bromophenyl)-2-(methylthio)thieno[2,3-d]pyrimidine-6-carboxylic acid N-tert-butylamide (TPY4) on the basal and TSH-stimulated TH production in cultured FRTL-5 thyrocytes and on basal and thyrotropin-releasing hormone (TRH)-stimulated TH levels in the blood of rats.
View Article and Find Full Text PDFIn vitro evaluation of silver-zinc oxide-eugenol nanocomposite for enhanced antimicrobial and wound healing applications in diabetic conditions.
Discov Nano
January 2025
Department of Biotechnology, Alagappa University, Karaikudi, 630003, India.
Diabetic wounds with chronic infections present a significant challenge, exacerbated by the growing issue of antimicrobial resistance, which often leads to delayed healing and increased morbidity. This study introduces a novel silver-zinc oxide-eugenol (Ag+ZnO+EU) nanocomposite, specifically designed to enhance antimicrobial activity and promote wound healing. The nanocomposite was thoroughly characterized using advanced analytical techniques, confirming its nanoscale structure, stability and chemical composition.
View Article and Find Full Text PDFPhenomenological Modeling of Antibody Response from Vaccine Strain Composition.
Antibodies (Basel)
January 2025
Department of Chemistry and Chemical Biology, Harvard University, Cambridge, MA 02138, USA.
The elicitation of broadly neutralizing antibodies (bnAbs) is a major goal of vaccine design for highly mutable pathogens, such as influenza, HIV, and coronavirus. Although many rational vaccine design strategies for eliciting bnAbs have been devised, their efficacies need to be evaluated in preclinical animal models and in clinical trials. To improve outcomes for such vaccines, it would be useful to develop methods that can predict vaccine efficacies against arbitrary pathogen variants.
View Article and Find Full Text PDFPeptide Inhibitor Assay for Allocating Functionally Important Accessible Sites Throughout a Protein Chain: Restriction Endonuclease EcoRI as a Model Protein System.
BioTech (Basel)
December 2024
The BCPH Unit of Molecular Physiology, Department of Chemistry, Biology and Marine Science, Faculty of Science, University of the Ryukyus, Nishihara 903-0213, Okinawa, Japan.
Functionally important amino acid sequences in proteins are often located at multiple sites. Three-dimensional structural analysis and site-directed mutagenesis may be performed to allocate functional sites for understanding structure‒function relationships and for developing novel inhibitory drugs. However, such methods are too demanding to comprehensively cover potential functional sites throughout a protein chain.
View Article and Find Full Text PDFNanoplastic-Induced Developmental Toxicity in Ascidians: Comparative Analysis of Chorionated and Dechorionated Embryos.
J Xenobiot
January 2025
Laboratoire de Biologie du Développement (LBDV), Institut de la Mer de Villefranche (IMEV), Sorbonne Université, Centre National de la Recherche Scientifique (CNRS), 06230 Villefranche-sur-Mer, France.
Nanoplastics pose a growing threat to marine ecosystems, particularly affecting the early developmental stages of marine organisms. This study investigates the effects of amino-modified polystyrene nanoparticles (PS-NH, 50 nm) on the embryonic development of , a model ascidian species. Both chorionated and dechorionated embryos were exposed to increasing concentrations of PS-NH so morphological alterations could be assessed with a high-content analysis of the phenotypes and genotoxicity.
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