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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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Related Experiment Video

Updated: May 11, 2026

Visualizing Membrane Ruffle Formation using Scanning Electron Microscopy

Visualizing Membrane Ruffle Formation using Scanning Electron Microscopy

Published on: May 27, 2021

Aggregation-mediated macromolecular uptake by a molecular transporter.

Makoto Inoue¹, Wenyong Tong, Jeffrey D Esko

¹Department of Chemistry and Biochemistry, University of California, San Diego , 9500 Gilman Drive, La Jolla, California 92093, United States.

ACS Chemical Biology

|April 30, 2013

Summary

Cellular uptake of streptavidin is enhanced by preincubating cells with biotinylated guanidinoneomycin (biotinGNeo). This suggests heparan sulfate proteoglycan aggregation is key for guanidinoglycoside-mediated endocytosis and macromolecule delivery.

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Area of Science:

Cellular Biology
Biochemistry
Drug Delivery

Background:

Endocytosis is crucial for cellular uptake of macromolecules, but its mechanisms are not fully understood.
Molecular transporters facilitate this process, yet specific internalization pathways require elucidation.

Discussion:

Investigated cellular uptake of streptavidin using biotinylated guanidinoneomycin (biotinGNeo).
Compared direct conjugate incubation versus preincubation with biotinGNeo, observing enhanced uptake with preincubation.
Utilized FRET studies to reveal streptavidin aggregation on cell surfaces correlated with increased uptake.

Key Insights:

Preincubation with biotinGNeo significantly enhances streptavidin cellular uptake.
Heparan sulfate proteoglycan aggregation is identified as a critical step for endocytosis mediated by guanidinoglycosides.
This pathway offers a general strategy for delivering diverse macromolecules into cells.

Outlook:

Potential for developing novel drug delivery systems targeting specific cellular uptake mechanisms.
Further research into guanidinoglycoside interactions with cell surface proteoglycans.
Exploration of this method for delivering larger biomolecules and therapeutic agents.