Cited by 129Drug Transport and Resistance MechanismsPharmacogenetics and Drug MetabolismAmino Acid Enzymes and Metabolism

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Organic Anion Transporters and Their Implications in Pharmacotherapy

Emami Riedmaier, Arian, Nies, Anne T., Schaeffeler, Elke, Schwab, Matthias·2012·Pharmacological Reviews

DOI 10.1124/pr.111.004614

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Abstract

Organic anion transporters play an essential role in the distribution and excretion of numerous endogenous metabolic products and exogenous organic anions, including a host of widely prescribed drugs. The expression and activity of these transporters is influenced by several conditions, including transcriptional regulation, gender-dependent regulation, and genetic variation. In addition, the interaction of these transporters with several drugs and endogenous substrates has been well documented and may play a significant role in drug disposition and development of various disease states, such as nephrotoxicity and familial idiopathic hypouricemia. Members of this family of transporters have been localized mainly to the renal epithelia of various species. Much of the early research in this field has focused on their role in renal drug transport, yet increasing research on this family of transporters has localized them to various other epithelial tissues, including liver, brain, and placenta. Thus, an understanding of the role of these transporters in drug interaction and disposition in the kidney and other tissues may help in the determination of individual drug response, susceptibility to drug toxicity, and chemical carcinogenesis. This review seeks to summarize current knowledge of the molecular function and substrate profile of cloned organic anion transporters and to discuss recent progress in the understanding of the impact of interindividual variability, transcriptional regulation, and tissue distribution on individual drug response.

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Authors: Emami Riedmaier, A., Nies, A. T., Schaeffeler, E., & Schwab, M.
Affiliations: Universitätsklinikum Tübingen (DE)
ORCID: Nies, Anne T.
Schaeffeler, Elke
Schwab, Matthias
Venue: Pharmacological Reviews
Publisher: Elsevier BV
Published: 2012-07
Volume: 64
Issue: 3
Pages: 421-449
ISSN: 0031-6997 (ISSN-L)
DOI: 10.1124/pr.111.004614
OpenAlex: W2114622644
Cited by: 128
References: 219
Citations by year: 2026: 4 · 2025: 4 · 2024: 10 · 2023: 9 · 2022: 7 · 2021: 7 · 2020: 7 · 2019: 11 · 2018: 6 · 2017: 13 · 2016: 12 · 2015: 11 · 2014: 18 · 2013: 8 · 2012: 1
FWCI: 1.26
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
Locations: Pharmacological Reviews (publishedVersion)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
Life Sciences › Biochemistry, Genetics and Molecular Biology › Biochemistry › Amino Acid Enzymes and Metabolism
Keywords: organic anion transporters, renal drug transport, drug disposition, drug-drug interactions, nephrotoxicity, transcriptional regulation, interindividual variability, genetic variation, tissue distribution, drug toxicity, chemical carcinogenesis, substrate specificity
MeSH terms: Animals, Biological Transport, Drug Interactions, Drug Therapy, Pharmaceutical Preparations, Female, Gene Expression Regulation, Humans, Male, Organ Specificity, Sex Characteristics, Substrate Specificity, Tissue Distribution, Xenobiotics, Organic Anion Transporters, Drug-Related Side Effects and Adverse Reactions

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Organic Anion Transporters and Their Implications in Pharmacotherapy

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