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Loss of OATP1B3 function causes Rotor syndrome: implications for potential use of inhibitors in cancer

Elias Pratt1, Tristan M Sissung, William D Figg

  • 1Clinical Pharmacology Program, Center for Cancer Research, National Cancer Institute; Bethesda, MD 20892, USA.

Cancer Biology & Therapy
|September 8, 2012
PubMed

Insights

Organic anion transporter proteins (OATPs) are increasingly recognized in cancer biology. While inhibiting OATP1B3 shows promise for prostate cancer, potential interference with normal functions and drug interactions warrants caution.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Organic anion transporter proteins (OATPs) are increasingly implicated in cancer cell biology.
  • De novo expression of OATPs is observed in various cancers, including breast, colon, pancreatic, gastric, and prostate cancer.
  • Polymorphisms in OATP1B3 affecting its function correlate with treatment outcomes in prostate cancer patients.

Purpose of the Study:

  • To explore the therapeutic potential of targeting OATP1B3 in cancer.
  • To evaluate the implications of OATP1B3 inhibition in prostate cancer treatment.
  • To address concerns regarding the safety and physiological impact of OATP1B3 inhibition.

Main Methods:

  • Review of existing literature on OATP expression in cancer.
  • Analysis of clinical data linking OATP1B3 polymorphisms to prostate cancer progression and survival.
  • Assessment of potential off-target effects and drug interactions associated with OATP1B inhibition.

Main Results:

  • OATP1B3 polymorphisms associated with reduced function correlate with improved outcomes in prostate cancer patients undergoing androgen deprivation therapy.
  • This improved outcome is potentially due to decreased testosterone uptake by tumors.
  • Therapeutic inhibition of OATP1B3 is proposed but faces challenges.

Conclusions:

  • OATP1B3 plays a significant role in prostate cancer biology and treatment response.
  • Targeting OATP1B3 offers a potential therapeutic strategy, particularly in prostate cancer.
  • Potential interference with normal OATP1B3 functions (e.g., bile acid and bilirubin transport) and unknown drug interactions necessitate careful consideration before clinical application.

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