Round Table Presentations Short Topic Presentations Academic Research Award Presentations Regular Poster Presentations Round Table Presentations Round Table 1: Transporters in Drug Discovery and Mechanistic PBPK Models Roundtable Chairs: Joanne Brodfuehrer and Stephen Wang (Pfizer) Abstract: Membrane transporters play important roles throughout drug development. Speakers will provide insights i...

Background: A major obstacle in the fight against cancer is development of drug resistance response to therapy. Metastatic Breast Cancer (MBC) extremely difficult cure, mainly because it driven by tumor cell subpopulations characterized an increased capacity adaptation various stresses. Emerging evidence suggests that epithelial-mesenchymal transition (EMT) program contributes resistance. There...

Entecavir (ETV) is one of the most potent agents for the treatment of the hepatitis B viral infection. The drug is principally eliminated by the kidney. The goal of this study was to investigate the potential of ETV to interact in vitro with the renal SLC transporters hOAT1, hOCT2, hCNT2 and hCNT3. Potential drug-drug interactions of ETV at the renal transporters with antiviral drugs known to b...

Nosocomial infections with Enterococcus faecalis are an emerging health problem. However, drug efflux pumps contributing to intrinsic drug resistance are poorly studied in this Gram-positive pathogen. In this study, we functionally investigated seven heterodimeric ABC transporters of E. faecalis that are annotated as drug efflux pumps. Deletion of ef0789-ef0790 on the chromosome of E. faecalis ...

ATP-binding cassette multidrug transporters are probably present in all living cells, and are able to export a variety of structurally unrelated compounds at the expense of ATP hydrolysis. The elevated expression of these proteins in multidrug resistant cells interferes with the drug-based control of cancers and infectious pathogenic microorganisms. Multidrug transporters interact directly with...

Drug delivery across the blood–brain barrier (BBB) has several challenges, especially toward targeting neurological diseases, due to tight and selective function of BBB. Several structural functional components this contribute restricting drug entry, such as interendothelial junctions (TJs), efflux transporters, drug-metabolizing enzymes, crosstalk between cells neurovascular unit. Among differ...

Numerous studies in the past 25 years have shown that most compounds, generated in metabolic processes (metabolic intermediates and products; endogenous compounds) or introduced orally or parenterally (nutritive compounds, medicaments, environmental toxins and other xenobiotics), do not enter or exit cells freely, by simple diffusion. Rather, their transmembrane movement is mediated by various ...

Among drug-induced renal failure, direct renal tubular toxicity, typically described as toxic acute tubular necrosis, is often associated with increased cellular uptake of nephrotoxic compounds. Drug transporters in tubular cells are the first fundamental stage in the development of the nephrotoxic process. Several examples can be given of organic substances that are nephrotoxic only after bein...

Transporters are membrane proteins that are present in all organisms. These proteins control the influx of essential nutrients and ions and the efflux of cellular waste, environmental toxins, and other xenobiotics. Consistent with their critical roles in cellular homeostasis, approximately 2000 genes in the human genome ~7 of the total number of genes code for transporters or transporter-relate...