Introduction Transporters are membrane proteins highly expressed in various organs of humans. They play a pivotal role in the absorption and disposition of both endogenous and exogenous molecules. In the […]
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Clinical Probes and Endogenous Biomarkers as Substrates for Transporter Drug-Drug Interaction Evaluation
Perspectives From the International Transporter Consortium Introduction Transporter studies are performed at various stages of drug development ‒ discovery to first-in-human (FIH) phase (in-vitro substrate and inhibition studies), FIH to […]
Silencing the Breast Cancer Resistance Protein Expression and Function in Caco-2 Cells Using Lentiviral Vector-Based Short Hairpin RNA
A series of stable breast cancer resistance protein (BCRP, ABCG2) knockdown cell lines were produced by transduction of Caco-2 cells with lentiviral vector-based short hairpin RNA (shRNA). Caco-2 cell is […]
Why evaluate the substrate and inhibitor potential of the investigational drug for specific transporters and why do the FDA and EMA care? Membrane transporters can have clinically relevant effects on […]