BLU-945 suppresses ABCB1-mediated drug efflux and restores chemosensitivity in multidrug-resistant cancer cells.

Carborane-Based Derivatives as Inhibitors of the Breast Cancer Resistance Protein (ABCG2).

Dihydroartemisinin overcomes cisplatin resistance in bladder cancer via suppression of the PI3K/AKT/ABCB1 signaling Axis

Cisplatin resistance substantially limits the efficacy of bladder cancer chemotherapy, and effective strategies to overcome resistance remain insufficient. In this study, we demonstrate that dihydroartemisinin (DHA) restores cisplatin sensitivity in resistant bladder cancer cells by suppressing the PI3K/AKT/ABCB1 sig...

Ebselen sensitizes multidrug-resistant cancer cells to doxorubicin by disrupting cellular redox homeostasis and inducing ferroptosis.

AIM Multidrug resistance (MDR), driven by P-glycoprotein (P-gp/ABCB1)-mediated drug efflux and enhanced antioxidant defenses, remains a major obstacle to effective chemotherapy. This study investigated whether thioredoxin reductase (TrxR) inhibition by ebselen induces ferroptosis, suppresses NRF2/Keap1 signaling and re...

Natural Molecules as Modulators of Drug Resistance: Emerging Strategies.

Cancer drug resistance remains a major challenge in oncology, limiting the long-term effectiveness of chemotherapy, targeted therapies, and immunotherapy. Resistance arises through multiple interconnected mechanisms, including overexpression of ATP-binding cassette (ABC) transporters, activation of pro-survival signali...

Identification of the Acetamide-Chalcone Derivative That Selectively Inhibits ABCG2 Transport Activity

Multidrug resistance (MDR) remains a major obstacle to effective cancer chemotherapy, often driven by the overexpression of ABC transporters such as ABCG2. In this study, we identified the synthetic chalcone derivative, B5, as a selective ABCG2 inhibitor. Among the 20 chalcone analogs evaluated, B5, bearing an acetamid...

SRPK1 is a determinant of chemoresistance to Docetaxel in prostate cancer

Docetaxel is a major therapeutic option for advanced prostate cancer, but the development of acquired resistance substantially limits its clinical efficacy. Although multiple mechanisms have been implicated in docetaxel resistance, the upstream regulatory pathways coordinating these phenotypes remain incompletely under...