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Transporter Screening Service

Transporter Screening Service

Transporters are membrane proteins that power the influx and efflux of numerous substances, including essential nutrients, ions, neurotransmitters, cellular waste, environmental toxins, and other xenobiotics such as drugs. Transport proteins are vital to the growth and life of all living organisms. There are several different kinds of transport proteins.

Transporter Screening Service

Drug transporters are composed of two major super families: ATP-binding cassette (ABC) transporter and solute carrier (SLC) transporter. ABC transporters directly rely on ATP hydrolysis to pump their substrates across membranes, thus acting as a primarily active transporter, which mediates unidirectional efflux. They mainly function 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 convey drugs using energy produced by transmembrane movement of other solutes in accordance with their concentration gradient. They are classified as facilitated transporters or secondary active transporters, mediating both drug uptake and efflux movements. These transporters play significant roles in hepatic and renal uptake and urinary excretion. Specifically, for some SLC transporters that are regarded as neurotransmitters, they are vital drug targets themselves with clinical drugs treating various psychiatric disorders.

Transporters involved in diseases such as depression, schizophrenia, cancer, and diabetes as potential therapeutic targets. Therefore, transporters screening plays an important role in identifying and verifying a drug’s clinical efficacy and safety.

Profacgen offers transporter targets that have great significance in preclinical study, including 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. 

Assays available:

1. Electrophysiology
2. Radioactive flux detection
3. Fluorescence detection

Profacgen provides a comprehensive package of services to facilitate your transporter screening study in preclinical drug development. We have specialized transporter panels and provide customized transporter-screening services, which will facilitate the discovery of novel transporter-targeted compounds. We have developed transporter panels including FDA transporter screening panel, monoamine transporter models and many other cell models. We provide robust transporter uptake and inhibition assays to perform quick and cost-effective screening of new molecular entities (NMEs) for their interactions with transporters, and present results with good signal-to-background ratio and Z’ scores.

Features:

  Cell based assays providing functional characterization of compound activity
  A wide coverage of key drug transporters and neurotransmitter transporters 
  Availability of various panels

 

Our available transporter targets and the screening assays we have developed so far are listed in the attached instruction manual.

 

Please contact us for more details of our preclinical transporter screening service. Our experts will provide you an optimal solution for your transporter-screening project and trouble-shooting for you throughout the whole process.

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