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Development of an Oral Epithelial Ex Vivo Organ Culture Model for Biocompatibility and Permeability Assessment of Biomaterials.
Bioengineering (Basel)
October 2024
Department of Oral Medicine/Pathology, School of Dentistry, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
In the present study, a customized device (Epi-ExPer) was designed and fabricated to facilitate an epithelial organ culture, allowing for controlled exposure to exogenous chemical stimuli and accommodating the evaluation of permeation of the tissue after treatment. The Epi-ExPer system was fabricated using a stereolithography (SLA)-based additive manufacturing (AM) method. Human and porcine oral epithelial mucosa tissues were inserted into the device and exposed to resinous monomers commonly released by dental restorative materials.
View Article and Find Full Text PDFPROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network.
Structure
December 2024
Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, 262 Danny Thomas Place, MS 1000, Memphis, TN 38105-3678, USA. Electronic address:
Article Synopsis
- - PROTACs are molecules designed to induce protein degradation by linking a target protein with an E3 ubiquitin ligase through a specialized linker, but small changes in the linker can significantly affect their effectiveness.
- - Researchers discovered dTAG-13, a PROTAC that activates the pregnane X receptor (PXR) but does not lead to protein degradation, indicating that different components affect the PROTAC's function.
- - A crystal structure analysis showed that the binding of ligands to PXR can cause structural changes in the binding pocket and disrupt E3 ligase complex formation, emphasizing the importance of the linker’s environment in PROTAC activity.
Development of a high throughput cytochrome P450 ligand-binding assay.
J Biol Chem
October 2024
Department of Pharmacology, University of Michigan, Ann Arbor, Michigan, USA; Departments of Medicinal Chemistry, and Biological Chemistry and the Programs in Chemical Biology and Biophysics, University of Michigan, Ann Arbor, Michigan, USA. Electronic address:
Article Synopsis
- * Traditional methods for studying these interactions are time-consuming and resource-intensive, but a new semi-automated high-throughput screening assay allows for significantly faster testing with less protein and solvents, validated for different substrate interactions.
- * The assay was used to screen a library of imidazole compounds across three different cytochrome P450 enzymes, yielding unique binding profiles that can help develop pharmacophores and identify potential inhibitors or new drug candidates while enhancing computational predictions.
Exploring the protective effect and mechanism of icariside II on the bladder in a rat model of radiation cystitis based on transcriptome sequencing.
Int J Radiat Biol
September 2024
Department of Urology, Beijing Friendship Hospital, Capital Medical University, Beijing, China.
Purpose: Radiation cystitis (RC) is a complex and common complication after radiotherapy for pelvic cancer. Icariside II (ICAII) is a flavonoid compound extracted from Epimedium, a traditional Chinese medicine, with various pharmacological activities. The aim of the present study was to investigate the cysto-protective effects of ICAII in RC rats and its possible mechanisms.
View Article and Find Full Text PDFAn Innovative Aggregation-Induced Emission-Based NIR Fluorescent Probe for Visualizing Carboxylesterases in Living Cells, Zebrafish, and Tumor-Bearing Mice.
Molecules
August 2024
Synergy Innovation Centre of Biological Peptide Antidiabetics of Hubei Province, College of Life Science, Wuchang University of Technology, Wuhan 430223, China.
Article Synopsis
- Carboxylesterases (CEs) are enzymes that are important for breaking down foreign substances and regulating fats in the body, and their abnormal levels are linked to diseases like diabetes and liver cancer.
- A new near-infrared (NIR) fluorescent probe has been developed to detect CEs quickly and accurately, with a rapid response time and high sensitivity.
- This probe can monitor changes in CE levels in living cells and zebrafish, and it has potential applications for imaging liver tumors and assisting in surgeries, making it valuable for medical diagnostics and research.
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