Bile Acid Uptake Transporters as Targets for Therapy

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Using Multi-fluorinated Bile Acids and In Vivo Magnetic Resonance Imaging to Measure Bile Acid Transport
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Published on: November 27, 2016

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Davor Slijepcevic1, Stan F J van de Graaf

  • 1Tytgat Institute for Liver and Intestinal Research, Academic Medical Center, Amsterdam, The Netherlands.

Digestive Diseases (Basel, Switzerland)
|March 2, 2017
PubMed
Abstract

Insights

Targeting bile acid transporters impacts glucose, lipid, and energy balance. Inhibiting uptake via NTCP or ASBT offers potential therapeutic strategies for metabolic homeostasis.

Area of Science:

  • Endocrinology and Metabolism
  • Hepatology
  • Gastroenterology

Background:

  • Bile acids are crucial signaling molecules regulating glucose, lipid, and energy homeostasis.
  • They exert effects via farnesoid X receptor (FXR) and TGR5 signaling pathways.
  • Bile acid transporters, including NTCP and ASBT, are key to bile acid circulation and signaling.

Purpose of the Study:

  • To review current understanding of targeting bile acid uptake transporters.
  • To explore the impact on systemic and intestinal bile acid dynamics.
  • To discuss emerging therapeutic applications.

Main Methods:

  • Literature review and synthesis of current research findings.
  • Analysis of pharmacological interventions targeting bile acid transporters.
  • Discussion of clinical trial data for ASBT inhibitors.

Main Results:

  • Modulation of NTCP and ASBT affects bile acid localization, dynamics, and signaling.
  • NTCP inhibition (e.g., myrcludex B) impacts hepatic bile acid uptake.
  • ASBT inhibitors are in clinical trials for modulating intestinal bile acid uptake.

Conclusions:

  • Targeting bile acid uptake transporters presents a promising therapeutic avenue.
  • Understanding transporter modulation is key to optimizing metabolic regulation.
  • Further research into systemic and intestinal bile acid dynamics is warranted for therapeutic development.

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