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Organic anion-transporting polypeptides: a novel approach for cancer therapy

Tianyu Liu1, Qingyong Li

  • 1State Engineering Laboratory of Bio-Resources Eco-Utilization, Northeast Forestry University, Ministry of Education , Harbin , China and.

Journal of Drug Targeting
|August 31, 2013
PubMed

Insights

Organic anion-transporting polypeptides (OATPs) are crucial transporters for drugs and nutrients. Their expression in tumors highlights their potential as anti-cancer drug targets.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Organic anion-transporting polypeptides (OATPs), encoded by SLCO genes, form a vital transporter superfamily.
  • They facilitate transmembrane transport of diverse drugs and endogenous compounds, including bile acids, hormones, and prostaglandins.
  • Eleven human OATPs exhibit distinct transport functions and tissue-specific expression patterns.

Purpose of the Study:

  • To review the role of OATPs in drug transport and their significance in cancer.
  • To highlight OATPs as potential biomarkers and therapeutic targets in oncology.

Main Methods:

  • Literature review of studies on OATP function, substrate specificity, and genetic polymorphisms.
  • Analysis of OATP expression in normal tissues and malignancies.
  • Evaluation of OATP involvement in the pharmacokinetics of clinical drugs.

Main Results:

  • OATPs transport numerous clinically relevant drugs, with OATP1B1, OATP1B3, OATP2B1, and OATP1A2 being key transporters.
  • Liver-specific OATP1B1 and OATP1B3, along with testis-specific OATP6A1, are upregulated in various cancers, serving as potential biomarkers.
  • Genetic variations in OATP genes influence substrate uptake and pharmacokinetics.

Conclusions:

  • OATPs are integral to drug and nutrient transport, with specific isoforms implicated in cancer progression.
  • Their expression in tumors and role in transporting anti-cancer drugs position OATPs as significant therapeutic targets for novel anti-cancer drug development.

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