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Updated: Apr 16, 2026

Author Spotlight: Exploring the Role of Ion Channels in Cancer: Characterization and Potential Treatment Approaches
Published on: June 16, 2023
Role of Organic Anion-Transporting Polypeptides (OATPs) in Cancer Therapy
Nilay Thakkar1, A Craig Lockhart, Wooin Lee
1Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, Kentucky, USA.
Abstract:
The superfamily of organic anion-transporting polypeptides (OATPs, gene symbol SLCO) includes important transporters handling a variety of endogenous and xenobiotic substrates. Currently, 11 human OATPs are known and their substrates include endogenous hormones and their conjugates, anticancer drugs, and imaging agents. The contribution of OATPs to the in vivo disposition of these substrates has been extensively investigated. An accumulating body of evidence also indicates that the expression of some OATPs may be up- or downregulated in several types of cancers, suggesting potential pathogenic roles during the development and progression of cancer. Given that the role of OATPs in handling cancer therapeutics has been already covered by several excellent reviews, this review will focus on the recent progresses on the topic, in particular the role of OATPs in the disposition of anticancer drugs, the impact of OATP genetic variations on the function of OATPs, and the OATPs differentially expressed in cancer and their potential roles in cancer development, progression, and treatment.
Insights
Organic anion-transporting polypeptides (OATPs) are crucial for drug disposition and cancer development. This review explores OATP roles in anticancer drug handling, genetic variations, and cancer-specific expression.
Area of Science:
- Pharmacology and Toxicology
- Molecular Biology
- Oncology
Background:
- Organic anion-transporting polypeptides (OATPs) are a superfamily of transporters involved in the uptake of diverse endogenous and xenobiotic substances.
- Known human OATPs (SLCO gene family) transport hormones, anticancer drugs, and imaging agents, influencing their in vivo distribution.
- Altered OATP expression is implicated in cancer development, progression, and response to therapy.
Purpose of the Study:
- To review recent advances in understanding the role of OATPs in cancer.
- To focus on OATP involvement in anticancer drug disposition, the impact of genetic variations, and their differential expression in cancer.
- To explore the potential roles of cancer-associated OATPs in tumorigenesis and treatment.
Main Methods:
- Literature review of recent scientific publications.
- Synthesis of data on OATP function, genetic polymorphisms, and cancer biology.
- Analysis of OATP expression patterns in various cancer types.
Main Results:
- OATPs significantly influence the pharmacokinetics and efficacy of numerous anticancer drugs.
- Genetic variations in OATP genes can alter transporter function, impacting drug response and toxicity.
- Specific OATPs are differentially expressed in cancers, correlating with disease progression and patient outcomes.
Conclusions:
- OATPs are critical players in cancer pharmacotherapy, affecting drug delivery and efficacy.
- Understanding OATP genetic variations and cancer-specific expression is vital for personalized cancer treatment strategies.
- Targeting OATPs presents a potential avenue for novel cancer therapies and improved drug utilization.
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