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.

The AAPS Journal
|March 5, 2015
PubMed

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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