Related Experiment Video
Updated: Jun 21, 2026
07:10
High-Throughput Expression and Purification of Human Solute Carriers for Structural and Biochemical Studies
Published on: September 29, 2023
Transporters and drug disposition
1Division of Clinical Pharmacology, 572 MRB1, Vanderbilt University School of Medicine, Nashville, TN 37323-6602, USA. richard.kim@mcmail.vanderbilt.edu
Current Opinion in Drug Discovery & Development
|August 4, 2009
Summary
Drug transporters significantly influence how the body processes and responds to medications, impacting drug disposition. Understanding these transport mechanisms alongside drug metabolism is crucial for accurate in vivo predictions.
Area of Science:
- Pharmacology
- Drug Metabolism and Transport
Background:
- Drug disposition and response variability cannot be solely explained by metabolism.
- Carrier-mediated transport processes play a critical role in drug absorption, distribution, and excretion.
Purpose of the Study:
- To review the role of drug transporters in intersubject variability of drug disposition.
- To discuss in vitro methodologies for assessing drug transporter expression in drug screening.
Main Methods:
- Literature review of drug transporter functions.
- Overview of in vitro drug transporter expression analysis techniques.
Main Results:
- Drug transporters are essential for understanding drug disposition alongside metabolism.
- In vitro transporter expression assays are relevant for drug screening.
Conclusions:
- Integrating transporter and metabolism data is vital for predicting in vivo drug behavior.
- In vitro transporter expression studies aid in drug development and screening.
More Related Videos
Related Concept Videos
01:14Hepatic Drug Clearance: Role of Transporters
In the liver and bile canaliculi, influx and efflux transporters modification can influence intrinsic clearance. Transporters play a significant role in moving drugs within liver cells. Elaborate models, such as the Biopharmaceutical Classification System (BCS), are essential to relate transporters to drug disposition. This system categorizes drugs into four classes based on solubility and permeability, providing insights into elimination routes and the effects of transporters following oral...
01:07Physiological Pharmacokinetic Models: Incorporating Hepatic Transporter-Mediated Clearance
Drug transporters are critical in drug absorption, distribution, and excretion processes. They should be included in physiological-based pharmacokinetic (PBPK) models, which help predict human drug disposition. However, predicting this is challenging during drug development, especially when liver transport is involved. However, with a realistic representation of body transport processes, an accurate model may be possible.
A recent model describes pravastatin's hepatobiliary excretion, mediated...
A recent model describes pravastatin's hepatobiliary excretion, mediated...
01:16Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters
The pharmacogenetics of drug transporters is increasingly recognized as a critical factor influencing interindividual variability in drug absorption, distribution, and elimination. These membrane-bound proteins regulate drugs' movement across cellular barriers by actively pumping them out (efflux) or facilitating their uptake (influx). Among the major transporter families, ATP-binding cassette (ABC) and solute carrier (SLC) transporters play particularly prominent roles. Genetic polymorphisms...
01:27Nonlinear Pharmacokinetics: Role of Transporters
A drug's nonlinear kinetics can be influenced by a diverse range of transporter proteins that serve as crucial players in drug distribution. These transporters, found within cells, can enhance or reduce local drug concentrations by facilitating the influx or efflux of drugs. For instance, the expression of xenobiotic transporters can be influenced by factors such as age and gender, potentially impacting the linearity of drug response.
Polymorphisms occurring in drug transporters can alter...
Polymorphisms occurring in drug transporters can alter...
01:06Carrier-Mediated Transport
Carrier-mediated transport is a pivotal process in drug absorption, particularly for lipid-insoluble drugs, and encompasses facilitated diffusion and active transport. Facilitated diffusion allows drugs to move along their concentration gradient without energy expenditure, while active transport utilizes ATP to drive drug movement against this gradient.
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
01:19Drug Absorption Mechanism: Carrier-Mediated Membrane Transport
Certain large, lipid-insoluble drug molecules that resemble amino acids, peptides, or glucose, require specialized carrier proteins to facilitate their diffusion across cell membranes. This transport can occur through either facilitated diffusion, which does not require energy input, or active transport, which does require energy input.
Facilitated diffusion is a passive process that utilizes human Solute Carrier (SLC) transporters. These transporters bind to the drug, undergo structural...
Facilitated diffusion is a passive process that utilizes human Solute Carrier (SLC) transporters. These transporters bind to the drug, undergo structural...