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Design of pH-responsive and amphiphilic pullulan-based biological macromolecule for gene delivery.
Int J Biol Macromol
January 2025
Institute of Organic Chemistry and Macromolecular Chemistry (IOMC), Friedrich Schiller University Jena, Humboldtstr. 10, D-07743 Jena, Germany; Jena Center for Soft Matters (JCSM), Friedrich Schiller University Jena, Philosophenweg 7, D-07743 Jena, Germany. Electronic address:
Nanomedicine, particularly gene delivery, holds immense potential and offers promising therapeutic options. Non-viral systems gained attention due to their binding capacity, stability and scalability. Among these, natural polysaccharides, such as pullulan, are advantageous in terms of sustainability, biocompatibility and potential degradability.
View Article and Find Full Text PDFUnraveling the synthetic strategy, structure activity relationship of azetidinones: Insights into their multidrug and toxin extrusion protein (MATE transporter) inhibition facilitating drug development against MDR.
Bioorg Chem
January 2025
Medicinal Chemistry Research Laboratory, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to be University), Campus-2, Ghatikia, Kalinga Nagar, Bhubaneswar, Odisha 751003, India. Electronic address:
Heterocyclic chemistry gathered a wide audience due to their presence in potential drug candidates and being attractive synthons initiating several retro-syntheses the organic as well as in medicinal chemistry fields. Among them, azetidinones have been a subject of discussion due to their serendipity, curiosity, versatility by Penicillin and Cephalosporins as β-lactam antibiotics. Despite possessing a large margin of biological activities, azetidinones mainly work as antimicrobial, interfering with bacterial cell-wall synthesis blocking transpeptidase.
View Article and Find Full Text PDFStructural insights into nucleocapsid protein variability: Implications for PJ34 efficacy against SARS-CoV-2.
Virology
January 2025
Department of Virology, Graduate School of Biomedical and Health Sciences, Hiroshima University, 1-2-3 Kasumi, Minami-ku, Hiroshima, 734-8551, Japan. Electronic address:
Human coronaviruses (HCoVs) include common cold viruses such as HCoV-229E, OC43, NL63 and HKU1 as well as MERS-CoV and SARS-CoV, which cause severe respiratory disease. Recently, SARS-CoV-2 caused a COVID-19 pandemic. The nucleocapsid (N) protein of coronaviruses, which is essential for RNA binding and homodimerization, has a highly conserved structure across viruses.
View Article and Find Full Text PDFThe development of α, β-unsaturated lactam-based andrographolide derivatives as anti-gastric cancer agents with the ability of inhibiting the ERK/c-Fos/Jun pathway.
Eur J Med Chem
January 2025
Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education and School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan, 450001, China. Electronic address:
Gastric cancer remains one of the global health threats for human beings. However, the therapeutic efficacy of the widely-used chemotherapy is usually limited due to the lack of specificity and the related toxicity. Only limited therapeutic agents were demonstrated to show selective and potent inhibitory activity to gastric cancer cells.
View Article and Find Full Text PDFQuantitative structure-activity relationship (QSAR) hazard assessment of the banned pesticides by the National Agency for Food and Drugs Administration and Control.
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Department of Biochemistry, University of Ilorin, Kwara State, Ilorin, Nigeria.
This study carried out a quantitative structure-activity relationship hazard assessment of the banned pesticides in Nigeria with a view of identifying the dangers posed by these pesticides. Structure-activity relationships (SARs) and quantitative structure-activity relationships (QSARs), which link a compound's chemical structure to its biological activity, can be used to create safer and more effective insecticides, prioritize chemicals for testing, and reduce the number of animal studies necessary throughout the regulatory process. The QSAR hazard assessment of the banned pesticides was carried out on the VEGA software.
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