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Updated: Jul 3, 2026

Functional Characterization of Na+/H+ Exchangers of Intracellular Compartments Using Proton-killing Selection to Express Them at the Plasma Membrane
07:38

Functional Characterization of Na+/H+ Exchangers of Intracellular Compartments Using Proton-killing Selection to Express Them at the Plasma Membrane

Published on: March 30, 2015

Physiology, structure, and regulation of the cloned organic anion transporters

C Srimaroeng1, J L Perry, J B Pritchard

  • 1Laboratory of Pharmacology, Environmental Toxicology Program, National Institute of Environmental Health Sciences, NC 27709, USA.

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
|August 1, 2008
PubMed

Insights

Organic anion transporters (OATs) are crucial for drug distribution and toxicity. This review details OAT properties, function, and factors influencing drug transport, highlighting remaining research questions.

Area of Science:

  • Pharmacology
  • Renal Physiology
  • Molecular Biology

Background:

  • Epithelial tissues, especially the kidney, utilize organic anion transporters (OATs) to manage the distribution, concentration, and retention of negatively charged drugs, xenobiotics, and metabolites.
  • OATs significantly influence the therapeutic efficacy and potential toxicity of these substances.
  • Understanding OATs is vital for predicting drug behavior and optimizing treatments.

Purpose of the Study:

  • To review the current knowledge on the properties and functional roles of cloned OATs.
  • To explore the structure-function relationships of OATs.
  • To identify factors affecting OAT-mediated transport efficacy.

Main Methods:

  • Literature review of cloned organic anion transporters.
  • Analysis of structure-function relationships.
  • Examination of factors influencing OAT activity, including protein binding, genetic variations, and expression regulation.

Main Results:

  • Significant advancements have been made in understanding OATs since the first cloning.
  • Key factors influencing OAT function include substrate protein binding, genetic polymorphisms, and transporter expression regulation.
  • The review synthesizes current data on OAT properties and roles.

Conclusions:

  • Despite progress, several questions regarding OATs remain unresolved.
  • Further research is needed on drug-drug interactions, newly cloned OATs, tissue-specific differences, and transporter regulation mechanisms.
  • Addressing these issues is crucial for a comprehensive understanding of OATs in drug disposition and toxicity.

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