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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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Drug Absorption Mechanism: Carrier-Mediated Membrane Transport01:19

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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...
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Cellular Membranes and Drug Transport01:24

Cellular Membranes and Drug Transport

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Drugs must traverse multiple biological barriers, such as multi-layered skin, single-layered intestinal epithelium, and the plasma membrane, to reach their target sites within the body. The plasma membrane, a highly structured composite of phospholipids, carbohydrates, and proteins, is the cell's protective boundary, facilitating selective substance exchange.
Phospholipids arrange themselves into a bilayer, with hydrophilic heads oriented outward and hydrophobic tails facing inward.
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Mechanisms of Drug Absorption: Paracellular, Transcellular, and Vesicular Transport01:23

Mechanisms of Drug Absorption: Paracellular, Transcellular, and Vesicular Transport

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Drugs need to permeate cell membranes to reach their target sites after administration. Orally administered drugs must transcend intestinal epithelial membrane barriers to infiltrate the systemic circulation. Drugs with a molecular weight of less than 500 Daltons diffuse through gaps between neighboring cells, called paracellular pathways.
However, most drugs use the transcellular route, traversing directly through the cell membranes via two mechanisms: passive and active transport. Passive...
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Facilitated Diffusion01:16

Facilitated Diffusion

536
The plasma membrane, a critical structure in cellular biology, houses an array of transporters, or carrier proteins, interspersed within its lipid bilayer. These proteins play a crucial role in solute transport through facilitated diffusion, a form of passive diffusion that uses transporters to move the molecules across the membrane.
In this process, substrates such as organic compounds and ions interact with a transporter on one side, triggering conformational changes in proteins that enable...
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Membrane Transporters01:31

Membrane Transporters

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Transporters are essential membrane transport proteins with functions related to cell nutrition, homeostasis, communication, etc. Approximately 7% of all genes in the human genome code for transporters or transporter-related proteins.
Transporters are mainly composed of alpha-helices, built from bundles of ten or more helices traversing the plasma membrane. The solute-binding sites are located midway, where some of the helices are broken or distorted, making space for the binding site through...
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Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
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Transporter-Mediated Drug Delivery.

Gergely Gyimesi1, Matthias A Hediger1

  • 1Membrane Transport Discovery Lab, Department of Nephrology and Hypertension, and Department for BioMedical Research, Inselspital, University of Bern, Freiburgstrasse 15, CH-3010 Bern, Switzerland.

Molecules (Basel, Switzerland)
|February 11, 2023
PubMed
Summary
This summary is machine-generated.

Solute carrier (SLC) proteins are key to cellular transport. Drug design leveraging SLC interactions can enhance therapeutic efficacy, bioavailability, and targeting, addressing current challenges in drug development.

Keywords:
SLCbile acidsdrug designmembrane transporternanoparticlepharmacokineticsprodrugsolute carrier

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Area of Science:

  • Cellular Biology
  • Pharmacology
  • Biochemistry

Background:

  • Transmembrane transport is crucial for cellular metabolism.
  • Solute carrier (SLC) proteins, a large superfamily, mediate this transport.
  • Xenobiotic interaction with SLCs impacts drug efficacy, bioavailability, and distribution.

Purpose of the Study:

  • To review drug design strategies targeting SLC transporters.
  • To explore nanoparticle-based approaches for enhanced drug delivery.
  • To identify future challenges and directions in SLC-targeted therapeutics.

Main Methods:

  • Literature review of drug design and SLC interactions.
  • Analysis of nanoparticle conjugation techniques for drug targeting.
  • Synthesis of current and future research trends in the field.

Main Results:

  • SLCs significantly influence xenobiotic pharmacokinetics.
  • Prodrug strategies and nanoparticle conjugation enhance drug targeting and absorption.
  • Exploiting SLC interactions offers a promising avenue for optimized drug therapy.

Conclusions:

  • Targeting SLC transporters is a viable strategy for improving drug efficacy and delivery.
  • Advanced therapeutic development requires addressing challenges in SLC-mediated transport.
  • Future research should focus on novel approaches for SLC-targeted drug design.