Drug Transporter Drug Discovery Assays
Drug transporters, which are found in a variety of organs including the intestine, brain, liver, and kidney, play an important role in the absorption, distribution, and excretion of pharmaceuticals and are one of the determinants of drug disposition. The degree of expression of each transporter subtype in each tissue and its corresponding substrate affinity determine the tissue distribution and elimination route of various medicines. Thus, controlling transporter function should allow for the rapid development of medicines with perfect pharmacokinetic profiles.
Creative Biolabs offers drug transporter drug discovery assays, as well as cutting-edge technology and scientific expertise to support your specific needs.
| Classification | Function | Subclassification |
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| ABC Transporter Assays | ABC transporters transport diverse substrates across cellular membranes using the energy of ATP binding and hydrolysis. The ABC transporter's membrane-spanning section protects hydrophilic substrates from the membrane bilayer's lipids, allowing them to cross the cell membrane. Both prokaryotes and eukaryotes have transporters, which act as pumps that expel poisons and medications from the cell. |
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| SLC Transporter Assays | The SLC transporters transported a wide range of solutes, including charged and uncharged organic molecules, inorganic ions, and the gas ammonia. |
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Pharmacology
Drug disposition is significantly influenced by drug transporters, which are expressed in many organs. In the future, it might be possible to create medications with the optimum pharmacokinetic profiles by controlling the activity of such transporters. The utilization of a transporter function allows a medicine to be delivered to a specific organ while avoiding distribution to other organs, managing the elimination process, and increasing oral bioavailability. It is useful to select a lead compound that may or may not interact with transporters, depending on whether such an interaction is desirable.
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Role of Transporters in Drug Absorption
The small intestine expresses a number of transporters that are crucial for the absorption of nutrients and endogenous substances. Drug absorption will be aided by the utilization of influx transporters expressed in the gut, such as organic anion transporting polypeptide-B (OATP-B/SLC21A9), apical sodium-dependent bile acid transporters (ASBT/SLC10A2), and oligopeptide transporters (PEPT1/SLC15A1). -
Role of Transporters in Tissue Distribution
Utilizing transporters to deliver drugs to target tissues: The transporters expressed in particular organs offer potential drug delivery targets. Pravastatin is the drug with the most thorough documentation, as transporters are required for oral absorption, hepatic uptake, and biliary excretion. Since the liver is the HMG-CoA reductase inhibitor's primary target, effective enterohepatic circulation is an important pharmacokinetic characteristic that helps to maximize the drug's therapeutic effects while reducing its adverse effects.
