ArticleEuropean journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences2012
Structural requirements of bile acid transporters: C-3 and C-7 modifications of steroidal hydroxyl groups.
Article in European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 33 citations in OpenAlex.
- Advances in Pharmacological Activities, Biosynthesis, and Structural Modification of Ursodeoxycholic Acid (UDCA): A Review.Drug design, development and therapy · 2025Review
- Structural modifications that increase gut restriction of bile acid derivatives.RSC medicinal chemistry · 2021Article
- Intestinal Absorption of Bile Acids in Health and Disease.Comprehensive Physiology · 2019Review
- Tyrosine Phosphorylation Regulates Plasma Membrane Expression and Stability of the Human Bile Acid Transporter ASBT (Molecular pharmaceutics · 2019Article
- Co-delivery doxorubicin and silybin for anti-hepatoma via enhanced oral hepatic-targeted efficiency.International journal of nanomedicine · 2019Article
- Liver-targeted delivery of insulin-loaded nanoparticles via enterohepatic circulation of bile acids.Drug delivery · 2018Article
- Advanced Prodrug Strategies in Nucleoside and Non-Nucleoside Antiviral Agents: A Review of the Recent Five Years.Molecules (Basel, Switzerland) · 2017Review
- Synthesis and Biological Evaluation of Bile Acid Analogues Inhibitory to Clostridium difficile Spore Germination.Journal of medicinal chemistry · 2017Article
- Synthesis and Evaluation of Bile Acid-Ribavirin Conjugates as Prodrugs to Target the Liver.Journal of pharmaceutical sciences · 2015Article
- Quantitative NTCP pharmacophore and lack of association between DILI and NTCP Inhibition.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2015Article
- Synthesis and in vitro evaluation of bile acid prodrugs of floxuridine to target the liver.International journal of pharmaceutics · 2014Article
- Design and evaluation of a novel trifluorinated imaging agent for assessment of bile acid transport using fluorine magnetic resonance imaging.Journal of pharmaceutical sciences · 2014Article
- Modern prodrug design for targeted oral drug delivery.Molecules (Basel, Switzerland) · 2014Article
- Key discoveries in bile acid chemistry and biology and their clinical applications: history of the last eight decades.Journal of lipid research · 2014Review
- Sodium-dependent bile salt transporters of the SLC10A transporter family: more than solute transporters.Pflugers Archiv : European journal of physiology · 2014Review
- Design and characterization of a novel fluorinated magnetic resonance imaging agent for functional analysis of bile Acid transporter activity.Pharmaceutical research · 2013Article
- Structure-activity relationship for FDA approved drugs as inhibitors of the human sodium taurocholate cotransporting polypeptide (NTCP).Molecular pharmaceutics · 2013Article
Corrections and comments
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2 authors at 1 institution in 1 country.
Funding
Abstract
The apical sodium dependent bile acid transporter (ASBT) and sodium-taurocholate cotransporting polypeptide (NTCP) are potential prodrug targets, but the structural requirements for these transporters are incompletely defined. The objective of this study was to evaluate the effect of C-3 and C-7 substitution on bile acid interaction with these bile acid transporters. Nineteen bile acid analogs were tested against ASBT and NTCP for binding, as well as translocation. Results indicated that ASBT and NTCP accommodated a wide range of substituents for binding, but all major C-7 modifications resulted in analogs that did not demonstrate active uptake by either ASBT or NTCP. A C-3 modification that was not tolerated at C-7 still afforded translocation via ASBT and NTCP, confirming the relative unacceptability of C-7 modification. Both ASBT and NTCP demonstrated a generally similar binding potency. Results suggest that drug conjugation to the C-3 hydroxyl group, rather than C-7, has potential to lead to a successful prodrug targeting ASBT and NTCP.
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Registered trials
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