BSEP and MRP2 Transport Vesicle Screening Assays for the Prediction of Potential Cholestatic and Drug-Induced Liver Injury
2 Jun 2014In this study, we examined 18 potential cholestatic drugs in human BSEP/MRP2 and rat Bsep/Mrp2 membrane vesicle assays. These drugs are known to be BSEP inhibitors, MRP2 inhibitors, dual BSEP and MRP2 inhibitors or glutathione depleters. The data suggest a relatively strong association between the interference with BSEP and/or MRP2 functions and drug-induced liver toxicity. These results demonstrate the applicability of in vitro, vesicle-based BSEP and MRP2 inhibition approaches to limit or avoid liver liabilities in humans that are not often detected by standard preclinical animal models.
Links
Tags
High-Throughput ScreeningHigh-throughput screening (HTS) is an automated drug discovery technique for identification of active compounds against a compound library. Use HTS readers and integrated assay preparation / analysis workstations to screen your compounds. Identify active compounds against various HTS libraries, including membranes, proteins and peptides and HTS cell lines. Find the best high-throughput screening products in our peer-reviewed product directory: compare products, check customer reviews and receive pricing direct from manufacturers.ADME-ToxicologyADME-toxicology (ADME-Tox) studies are used in pharmacology and pharmacokinetics to assess the activity/toxicity of drugs <i>in vivo</i> or <i>in vitro</i>. Find bioassays for absorption, distribution, metabolism, and excretion of drug molecules including cytotoxicity, transporter/permeability, metabolism and activity assays as well as hepatocytes and cell lines for ADME. Find the best ADME-toxicology products in our peer-reviewed product directory: compare products, check customer reviews and receive pricing direct from manufacturers.Medicinal ChemistryMedicinal chemistry is a broad discipline encompassing the design, identification, synthesis and development of chemicals in drug discovery. It includes a number of techniques covering structural biology, synthetic chemistry and molecular biology. Technologies used in medicinal chemistry include ADME, lab-on-a-chip, high content screening and assay assembly.Cell-Based AssaysCell-based assays are used to monitor the presence, quantity and activities of a desired cellular analyte including drug molecules or biomarkers. This can reveal information on cell health (apoptosis, cytotoxicity, viability and proliferation assays), cell metabolism, cell migration and cell signaling mechanisms. Find the best cell-based assay products, kits and equipment with our peer reviewed product directory: compare products, check customer reviews and receiving pricing direct from manufacturers.Liver DiseaseDrug MetabolismDrug metabolism is the enzymatic conversion within the body of pharmaceutical substances into other chemical compounds. The primary site for drug metabolism is the liver.