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Related Concept Videos

Drug Absorption Mechanism: Carrier-Mediated Membrane Transport01:19

Drug 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.
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Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

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Cellular Membranes and Drug Transport

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Carrier-Mediated Transport01:06

Carrier-Mediated Transport

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Determination of the Transport Rate of Xenobiotics and Nanomaterials Across the Placenta using the ex vivo Human Placental Perfusion Model
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Prostaglandin transport.

Victor L Schuster1

  • 1Departments of Medicine and Physiology & Biophysics, Albert Einstein College of Medicine, Bronx, NY 10461, USA. schuster@aecom.yu.edu

Prostaglandins & Other Lipid Mediators
|November 16, 2002
PubMed
Summary
This summary is machine-generated.

Prostaglandin transporters facilitate cellular uptake and clearance, regulating levels and receptor interactions. Key transporters like PGT, OATs, and MRPs are crucial for prostaglandin (PG) metabolism and function.

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Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
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Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers

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Area of Science:

  • Biochemistry
  • Cell Biology
  • Pharmacology

Background:

  • Newly synthesized prostaglandins (PGs) exit cells via simple diffusion.
  • Metabolic clearance of PGs necessitates energy-dependent cellular uptake and subsequent oxidation.
  • Several prostaglandin transporter proteins have been identified and characterized.

Purpose of the Study:

  • To elucidate the roles of various transporters in prostaglandin (PG) cellular uptake, efflux, and metabolic clearance.
  • To understand the functional characteristics and expression patterns of PG transporters.
  • To explore the implications of PG transport in regulating pericellular PG levels and receptor interactions.

Main Methods:

  • Cloning and characterization of prostaglandin transporter genes.
  • Analysis of transporter expression in relation to cyclooxygenase (COX) activity.
  • Investigating the substrate specificity and transport mechanisms of identified transporters (PGT, OATPs, OATs, MRPs).

Main Results:

  • Prostaglandin Transporter (PGT) is expressed in COX-positive cells, functions as a lactate/PG exchanger, and is co-regulated with COX.
  • Other transporters, including OATP family members and Organic Anion Transporters (OATs), also mediate PG uptake with varying affinities.
  • Multidrug Resistance-associated Proteins (MRPs) actively extrude glutathione-conjugated PGs, contributing to metabolic clearance.

Conclusions:

  • PGT plays a significant role in regulating pericellular PG levels through re-uptake and may influence PG interactions with specific receptors.
  • OATs are likely involved in the uptake of PGs for degradation and excretion in the kidneys and liver.
  • MRPs contribute to the metabolic clearance of PGs by actively transporting conjugated forms out of cells.