Transporters

Transporters, or transport proteins, are integral transmembrane proteins that assist in the movement of ions, nutrients, metabolites, small molecules, or macromolecules across biological membranes. Transport includes two different types: passive transport and active transport. The difference is that the former requires no energy while the latter requires energy. Transporters may mediate influx or efflux, and play a role in bringing drugs across biological membranes. They can expel drugs back to the external medium or to the blood.

Transporters are vital to the growth and life of all living organisms. And it is recognized that transporters are important for absorption, distribution and excretion of many drugs. Therefore, transporters are one of the most common classes of targets, and are commonly targeted by antihypertensive drugs, diuretics, anaesthetics and anti-arrhythmic drugs. Many genetic diseases involve defects in transporters in a particular substance or group of cells. An example of such disease is cystinuria, which involves defective cysteine transporters in the kidney cell membranes and causes urinary stones.

Simplified overview of human transport protein families. Figure1. Simplified overview of human transport protein families. (Viereck, M., et al., 2017)

Creative Biolabs provides a comprehensive target validation services to help confirm various types of transporters as therapeutic targets of drug discovery process thus to deal with data reproducibility crisis which is a big obstacle for drug research and development and may lead to failure and high risk of investment.

Creative Biolabs provides a comprehensive list of assays on multiple high-quality platforms to characterize the features of different transporters as your drug targets to advance your drug discovery. With experienced experts and cutting-edge technologies, we can provide high-quality and reliable services in a time-saving and cost-efficient manner. We offer professional target validation services for the following types of transporters.

ATP-Binding Cassette (ABC) Transporters

The ATP-binding cassette transporters (ABC transporters) are a transport system superfamily represented from prokaryotes to humans. ABC transporters are usually composed of multiple subunits containing transmembrane proteins and membrane-associated AAA ATPases. The ATPase subunit utilizes the energy of ATP binding and hydrolysis to provide the energy needed for transmembrane translocation of substrates, either for uptake or for export of the substrate. ABC transporters are known to play a crucial role in the development multidrug resistance (MDR), which can affect drug pharmacokinetics properties.

Solute Carrier (SLC) Transporters

The solute carrier transporters (SLC transporters) are a group of membrane transport proteins and are the second largest family of membrane proteins after G protein-coupled receptors (GPCRs). SLC transporters usually mediate the influx of substances across the cell membrane. They play an important role in physiological processes ranging from the cellular uptake of nutrients to the absorption of drugs and other xenobiotics. SLC transporters are important targets for drug development. Some well-known SLC transporters, such as neurotransmitter transporters, are the target of several marketed drugs. Numerous studies on SLC transporters indicate their new therapeutic opportunities in both rare and common diseases.

F-Type, V-Type and P-Type ATPases

F-Type, V-Type and P-Type ATPases are major classes of transport ATPases. Their main functions are moving many different types of ions or molecules across biological membranes. F-type ATPases synthesize ATP using a proton gradient and work in the reverse to use the energy gained from ATP hydrolysis to create a proton gradient. V-type ATPases also can hydrolyse ATP to drive a proton pump, but cannot work in reverse to synthesize ATP. The function of P-type ATPases is to transport various compounds, including ions and phospholipids, across membranes using ATP hydrolysis for energy. Different forms of ATPases have evolved over time to meet specific demands of cells. They are involved many important intracellular and intercellular processes, such as homeostasis, receptor-mediated endocytosis, active transport of metabolites, and neurotransmitter release. They are therefore attractive drug targets.

Creative Biolabs has a dedicated assay development team that will work closely with you to design customized assays for your specific drug target. Our service will meet your specific needs fast at extremely competitive prices. If you need more information, please feel free to contact us at anytime. We look forward to working with you and helping your drug research and development project succeed.

Reference

  1. Viereck, M., et al., 2017. Insights into Transporter Classifications: an Outline of Transporters as Drug Targets. Transporters as Drug Targets. Wiley‐VCH Verlag GmbH & Co. KGaA.
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