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[Reversal Roles and Its Mechanism of Asiatic Acid on Multidrug Resistance in K562/ADR Cells Through the Wnt/β-catenin Pathway].
Zhongguo Shi Yan Xue Ye Xue Za Zhi
December 2024
Department of Pediatrics， Binzhou Medical University Hospital， Binzhou 256603, Shandong Province， China.
Article Synopsis
- The study aimed to explore how asiatic acid (AA) affects the drug resistance in human leukemia cells (K562/ADR) resistant to adriamycin (ADR).
- AA was found to reduce the resistance of these cells and enhance the effectiveness of ADR, as shown by various assays including CCK-8 and flow cytometry.
- The results indicated that AA down-regulates the expression of certain proteins related to drug resistance, suggesting a potential mechanism for reversing resistance in these cancer cells.
Dynamic P-glycoprotein expression in early and late memory states of human CD8 + T cells and the protective role of ruxolitinib.
Biomed Pharmacother
December 2024
Department of Biophysics and Cell Biology, Faculty of Medicine, University of Debrecen, Debrecen 4032, Hungary; Doctoral School of Molecular Cell and Immune Biology, University of Debrecen, Debrecen 4032, Hungary; Dean's office, Faculty of Pharmacy, University of Debrecen, Debrecen 4032, Hungary. Electronic address:
ABCB1/MDR-1/P-glycoprotein (Pgp) is an ABC transporter responsible for cancer cell multi-drug resistance. It is expressed in cytotoxic T lymphocytes (CTL). Eliminating sensitive cancer cells during high-dose chemotherapy can also damage immune cells.
View Article and Find Full Text PDFCurcumin and doxorubicin encapsulated in biocompatible clay-based nanomaterial: A strategy to overcome multidrug resistance.
Arch Pharm (Weinheim)
January 2025
Dipartimento di Scienze Chimiche (DSC), Università di Catania, Catania, Italy.
Multidrug resistance (MDR) due to the overexpression of the P-glycoprotein (P-gp) efflux pump remains a significant challenge in cancer therapy, also in breast cancer. Traditional pharmacological approaches have focused on using inhibitors to modulate P-gp expression and function. Curcumin, a polyphenol derived from Curcuma longa L.
View Article and Find Full Text PDFFucosyltransferase 4 upregulates P-gp expression for chemoresistance via NF-κB signaling pathway.
Biochim Biophys Acta Gen Subj
December 2024
Division of Regulatory Glycobiology, Graduate School of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Japan; Institute of Molecular Biomembrane and Glycobiology, Tohoku Medical and Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai, Miyagi 981-8558, Japan. Electronic address:
Article Synopsis
- Multidrug resistance (MDR) complicates the development of effective chemotherapy, with previous research showing that GnT-III expression decreases chemoresistance and that fucosylation is heightened in resistant cell models.
- Using advanced techniques like CRISPR/Cas9, this study created a FUT4 knockout cell line to assess how fucosylation affects drug resistance by analyzing various gene expressions and drug response.
- The findings revealed that knocking out FUT4 lowered P-glycoprotein levels and enhanced drug sensitivity, indicating that FUT4 plays a pivotal role in regulating P-glycoprotein expression through the NF-κB signaling pathway, positioning it as a potential target for overcoming MDR in cancer treatment.
The "specific" P-glycoprotein inhibitor zosuquidar (LY335979) also weakly inhibits human organic cation transporters.
Naunyn Schmiedebergs Arch Pharmacol
December 2024
Internal Medicine IX - Department of Clinical Pharmacology and Pharmacoepidemiology, Heidelberg University, Medical Faculty Heidelberg, Heidelberg University Hospital, Im Neuenheimer Feld 410, 69120, Heidelberg, Germany.
Zosuquidar (LY335979) is a widely used experimental P-glycoprotein (P-gp) inhibitor, which is commended as very potent but also as very specific for P-gp. In this in vitro and in silico study, we demonstrated for the first time that zosuquidar also inhibits organic cation transporters (OCT) 1-3, albeit less potently than P-gp. This still has to be kept in mind when zosuquidar is used to inhibit cellular efflux of P-gp substrates that are concurrently transported into the cells by OCTs.
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