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Related Concept Videos

Carrier-Mediated Transport01:06

Carrier-Mediated Transport

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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...
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ABC Transporters: Exporter01:31

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ATP-binding cassette or ABC transporter is the largest superfamily of integral membrane proteins. The transporters have transmembrane-binding domains (TMDs) and nucleotide-binding domains (NBDs). The TMDs are specific to their substrates, whereas the NBDs are similar to engines that complete ATP hydrolysis to complete the substrate transport. They can be full transporters consisting of two TMDs and NBDs, half transporters with one TMD and NBD, while some encoded with a single TMD or NBD are...
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The Significance of Membrane Transport01:44

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The transport of solutes across the cell membrane is essential for metabolic processes, like maintaining cell size and volume, generating the action potential, exchanging nutrients and gases, etc. Membrane transport can be either passive or active. It can be simple diffusion, facilitated, or mediated transport aided by transport proteins such as transporters and channels.
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ABC Transporters: Importer01:27

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ATP-binding cassette or ABC transporters are a class of ATP-driven pumps that hydrolyze ATP to move solutes across the membrane. They can be grouped into importers and exporters. While exporters are present in all domains of life, importers exist only in bacteria and some plants.
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Pharmacogenetics of Drug Transporters: P-Glycoprotein and Solute Carrier Transporters01:16

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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...
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Drug Elimination by Renal Route: Tubular Secretion01:15

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Once the process of glomerular filtration is completed, blood carrying unfiltered drug molecules traverses through efferent arterioles and makes its way into the peritubular capillaries in the proximal tubule. A variety of carriers play a pivotal role in actively secreting drugs from these peritubular capillaries into the tubular fluid. The organic anion transporter transfers acidic drugs, against an electrochemical gradient, from the peritubular capillaries into the renal tubule cells and...
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Related Experiment Video

Updated: Apr 27, 2026

Expression, Detergent Solubilization, and Purification of a Membrane Transporter, the MexB Multidrug Resistance Protein
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Expression, Detergent Solubilization, and Purification of a Membrane Transporter, the MexB Multidrug Resistance Protein

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Substrate binding to the multidrug transporter MepA.

Christian Banchs1, Sandra Poulos1, Waroot S Nimjareansuk1

  • 1Department of Molecular Physiology and Biological Physics, University of Virginia School of Medicine, Charlottesville, VA, 22903, United States.

Biochimica Et Biophysica Acta
|June 27, 2014
PubMed
Summary

MepA transporter

Keywords:
Detergent effectDrug designDrug resistanceEffluxMembrane proteins

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Area of Science:

  • Microbiology
  • Molecular Biology
  • Biochemistry

Background:

  • MepA from Staphylococcus aureus is a multidrug transporter.
  • It confers multidrug resistance by exporting hydrophobic substrates.
  • Understanding MepA's substrate recognition is crucial for combating antibiotic resistance.

Purpose of the Study:

  • To investigate the substrate binding characteristics of the MepA transporter.
  • To determine the dissociation constants (KD) for MepA with acriflavine, rhodamine 6G, and ethidium.
  • To assess the influence of detergent micelles on MepA-substrate interactions.

Main Methods:

  • Measurement of dissociation constants (KD) for MepA-substrate interactions.
  • Evaluation of substrate binding in the presence of varying detergent concentrations.
  • Analysis of the binding affinity of an inactive D183A mutant.

Main Results:

  • All tested substrates (acriflavine, rhodamine 6G, ethidium) interact with detergent micelles.
  • The effect of detergent on KD is substrate-specific: R6G affinity is highly affected, while Acr and Et are modestly affected.
  • The D183A mutant exhibited reduced binding affinity for acriflavine and ethidium.

Conclusions:

  • Detergent micelles significantly influence the measured binding affinities of MepA substrates.
  • MepA's substrate recognition mechanism is complex and affected by the experimental environment.
  • The D183A mutation impacts MepA's ability to bind certain substrates, providing insights into its active site.