Transporters are a group of specialized membrane proteins that power the translocation of numerous substances, including essential nutrients, ions, neurotransmitters, cellular waste and environmental toxins, across the cellular membrane. Many transporters have emerged as therapeutic targets for diseases such as depression, schizophrenia, cancer, and diabetes. Therefore, transporter screening for therapeutically effective and safe compounds has become very important in the discovery and development of transporter-targeted drugs.
Schematic Diagram of Transporters [1]
Profacgen provides specialized transporter panels and customized transporter screening services enabling you to identify novel transporter-targeted compounds. Our transporter panels include FDA transporter screening panel, monoamine transporter models and many other cell models. We employ robust transporter uptake and inhibition assays to perform quick and cost-effective screening of new molecular entities (NMEs) for their interactions with transporters, and offer you results with good signal-to-background ratio and Z’ scores.
Assays:
- Electrophysiology
- Radioactive flux detection
- Fluorescence detection
Features:
- Cell based assays providing functional characterization of compound activity
- Coverage of key transporters
- Availability of various panels
- Short turn-around time
- Customized screening project design
Transporters involved in drug delivery and metabolism are classified into two major super families: ATP-binding cassette (ABC) transporter and solute carrier (SLC) transporter. ABC transporters function by coupling the hydrolysis of ATP with the transportation of specific substrates. They play important roles in hepatobiliary and urinary excretion of drugs, intestinal absorption of drugs, and in blood-brain barrier penetration of drugs. SLC transporters regulate drug influx and efflux, and can act as facilitated transporters or secondary active transporters, which transport drugs using energy produced by transmembrane movement of other solutes down 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 for the treatment of various psychiatric disorders.
Please feel free to contact us for more details about our customized transporter screening service.
Profacgen offers transporter targets that have great significance in clinical therapy, such as ATP binding cassette transporter (P-gp), neurotransmitter (SERT, DAT, NET), and solution carrier family transporter (SLC13). Our assay methods include radio-isotopic detection, fluorescence detection and ion flux detection.
See the instruction of transporter screening service. Find the targets list available in our screening service and the assay format we could provide to you.
Click here to download the Service Instruction.
References:
[1] G. Diallinas. Understanding Transporter Specifity and the Discrete Appearance of Channel-Like Gating Domains in Transporters. Front Pharmacol, 2014, 12 (5): 207.
