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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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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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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.
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Author Spotlight: Expression and Purification of Human Solute Carrier Transporters Using Codon-Optimized Genes
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Effect of Disease Pathologies on Transporter Expression and Function.

Amandla Atilano-Roque1, Gavriel Roda1, Uma Fogueri1

  • 1Department of Pharmaceutical Sciences, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of Colorado, Aurora, CO, USA.

Journal of Clinical Pharmacology
|July 8, 2016
PubMed
Summary
This summary is machine-generated.

Drug transporters in the liver, kidney, and brain are crucial for drug disposition. Disease significantly alters these transporter proteins, impacting drug efficacy and safety.

Keywords:
brainkidney diseaseliver diseasetransporters

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Area of Science:

  • Pharmacology
  • Biochemistry
  • Toxicology

Background:

  • Drug transporters are key to drug absorption, distribution, metabolism, and excretion (ADME).
  • Their localization in the liver, kidney, and brain is critical for clinical drug disposition and toxicology.
  • Disease states are increasingly recognized to affect drug-metabolizing enzymes and transporter proteins.

Purpose of the Study:

  • To review the role of uptake and efflux transporter proteins in the liver, kidney, and brain.
  • To discuss the mechanisms by which disease alters transporter expression and function.

Main Methods:

  • Literature review of studies on drug transporters in liver, kidney, and brain.
  • Analysis of mechanisms underlying disease-induced alterations in transporter expression and function.

Main Results:

  • Uptake and efflux transporters in the liver, kidney, and brain are significantly impacted by disease.
  • Disease can alter both the expression levels and functional activity of these vital transporter proteins.

Conclusions:

  • Altered drug transporter function due to disease has significant clinical implications for drug therapy.
  • Understanding these disease-related changes is essential for predicting drug disposition and toxicity.