Eurofins Discovery has developed a series of robust and validated assays to enable rapid and cost-effective screening of new molecular entities (NMEs) interacting with transporters for drug discovery purposes – and for further analysis of drug (ADME-Toxicology) and neurotransmitter transporters.
Transporters are membrane proteins that control the influx and efflux of essential nutrients, ions, neurotransmitters, cellular waste, environmental toxins, and other xenobiotics such as drugs. Drug transporters are composed of two major superfamilies: ABC (ATP binding cassette) and SLC (solute carrier) transporters.
ABC transporters mediate unidirectional efflux and are primarily active transporters as they directly rely on ATP hydrolysis to pump their substrates across membranes. They play major roles in hepatobiliary and urinary excretion of drugs from the blood to the lumen, intestinal absorption of drugs, and in brain blood barrier penetration of drugs. SLC transporters mediate either drug uptake or efflux and can be facilitated transporters or secondary active transporters, which transport drugs using energy produced by the transmembrane movement of other solutes in accordance with their concentration gradient. They play major roles in hepatic and renal uptake, and urinary excretion. Some SLC transporters, such as those for neurotransmitters, are also important drug targets themselves with clinical drugs treating various psychiatric disorders. Transporters play also a significant role in a drug’s clinical efficacy and safety.
Benefits of our transporter screening solutions
- Binding and cell-based assays (including transporter uptake and inhibition assays) to identify promising chemical leads and fully characterize their activity, potency and selectivity
- Key drug transporters and neurotransmitter transporters covered
- Drug transporter assays compatible with regulatory requirements
