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Development of multifunctional fluorescence-emitting potential theranostic agents for Alzheimer's disease.
Talanta
January 2025
Pharmaceutical Chemistry Research Laboratory I, Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi, 221005, India. Electronic address:
The cholinergic deficits and amyloid beta (Aβ) aggregation are the mainstream simultaneously observed pathologies during the progression of Alzheimer's disease (AD). Deposited Aβ plaques are considered to be the primary pathological hallmarks of AD and are contemplated as promising diagnostic biomarker. Herein, a series of novel theranostic agents were designed, synthesised and evaluated against cholinesterase (ChEs) enzymes and detection of Aβ species, which are major targets for development of therapeutics for AD.
View Article and Find Full Text PDFSkin disease-associated GJB4 variants differentially influence connexin stability, cell viability and channel function.
J Physiol
January 2025
Department of Physiology and Pharmacology, University of Western Ontario, London, ON, Canada.
Here we characterize seven Cx30.3 gene variants (R22H, S26Y, P61R, C86S, E99K, T130M and M190L) clinically associated with the rare skin disorder erythrokeratodermia variabilis et progressiva (EKVP) in tissue-relevant and differentiation-competent rat epidermal keratinocytes (REKs). We found that all variants, when expressed alone or together with wildtype (WT) Cx30.
View Article and Find Full Text PDFProbing Native CB2 Receptor Mobility in Plasma Membranes of Living Cells by Fluorescence Recovery After Photobleaching.
Chembiochem
January 2025
University of Teramo: Universita degli Studi di Teramo, Veterinary Medicine, Piano d'Accio snc, 64100, Teramo, ITALY.
In this study, we employed a novel fluorescent probe, RO7304924-which selectively targets cannabinoid 2 receptor (CB2R)-to assess the lateral mobility of CB2R within the plasma membrane of Chinese hamster ovary cells stably expressing a functional, untagged receptor variant. Utilizing confocal fluorescence recovery after photobleaching (FRAP), we quantified the diffusion coefficient and mobile fraction of CB2R, thereby demonstrating the efficacy of RO7304924 as an innovative tool for elucidating the dynamics of this major endocannabinoid-binding G protein-coupled receptor. Our present findings highlight the potential of combining advanced ligand-based fluorescent probes with FRAP for future investigations into the biochemical details of CB2R mobility in living cells, and its impact on receptor-dependent cellular processes.
View Article and Find Full Text PDFNorfloxacin Fluorescent Probe for the Assessment of Cefepime in Biological Fluids and Pharmaceutical Formulation; Investigation of the Greenness and Blueness Characteristics.
Luminescence
January 2025
Department of Chemistry, College of Science, Jouf University, Sakaka, Aljouf, Saudi Arabia.
In the present study, a norfloxacin (NFX) fluorescent probe was tailored for the spectrofluorometric measurement of cefepime (CFP). The proposed approach measured the quenching effect of CFP on the fluorescence intensity of NFX in acetate buffer solution. The obtained results show that CFP strongly quenches the fluorescence of NFX in a static mechanism.
View Article and Find Full Text PDFNaphthalimide and Carbazole Based Mechanochromic Molecular Dyads and Triads for Selective Lysosome Imaging.
Chem Asian J
January 2025
IISc: Indian Institute of Science, Inorganic and Physical Chemistry, Indian Institute of Science Bangalore, 560012, Bangalore, INDIA.
In this study, we report the design and development of a stable fluorescent probe that is selectively localized in the cytosol of Hela cells. We designed two probes, 1 and 2, with D-π-A (carbazole (Cbz)-vinyl-naphthalimide (NPI)) and A-π-D-π-A (NPI-vinyl-Cbz-vinyl-NPI) architecture, respectively. Probes 1 and 2 exhibit broad photoluminescence (PL) spectra ranging from green (550 nm) to far-red (800 nm) in solutions and aggregated states.
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