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Pharmacological and physiological functions of the polyspecific organic cation transporters: OCT1, 2, and 3

Johan W Jonker1, Alfred H Schinkel

  • 1The Netherlands Cancer Institute, Division of Experimental Therapy, Amsterdam, The Netherlands. h.jonker@nki.nl

The Journal of Pharmacology and Experimental Therapeutics
|October 25, 2003
PubMed

Insights

The body uses organic cation transporters (OCTs) to eliminate toxins and waste. Genetic variations in OCT1 and OCT2 influence how individuals respond to cationic drugs.

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Toxicology

Background:

  • The human body utilizes broad-specificity transporters for eliminating environmental toxins and metabolic waste.
  • Polyspecific organic cation transporters (OCTs) 1, 2, and 3 (SLC22A1-3) facilitate the transport of diverse organic cations, including drugs and toxins.
  • OCT1 and OCT2 are primarily located in the liver, kidney, and intestine, while OCT3 plays a role in peripheral monoamine neurotransmitter elimination.

Purpose of the Study:

  • To investigate the role of organic cation transporters (OCTs) in the elimination of toxins and metabolic waste.
  • To understand the impact of OCTs on the pharmacological behavior of substrate organic cations.
  • To explore the potential influence of genetic variations in OCT1 and OCT2 on interpatient drug response.

Main Methods:

  • Utilized knockout mouse models to demonstrate the functional significance of OCTs.
  • Investigated the transport activity of various substrate organic cations mediated by OCTs.
  • Identified and analyzed polymorphic genetic variants of human OCT1 and OCT2.

Main Results:

  • Knockout mouse studies confirmed the significant impact of OCTs on the pharmacological behavior of organic cations.
  • Polymorphic genetic variants in human OCT1 and OCT2 were found to severely affect transporter activity.
  • Variable activity of these transporters is suggested to contribute to interpatient differences in drug response.

Conclusions:

  • Organic cation transporters (OCTs) are crucial for the elimination of xenobiotics and endogenous compounds.
  • Genetic variability in OCT1 and OCT2 can lead to significant differences in drug efficacy and toxicity.
  • Understanding OCT function and genetics is vital for personalized medicine and optimizing drug therapy.

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