Functional characterization of cholera toxin inhibitors using human intestinal organoids

Domenique D. Zomer-Van Ommen, Aliaksei V. Pukin, Ou Fu, Linda H C Quarles Van Ufford, Hettie M. Janssens, Jeffrey M. Beekman, Roland J. Pieters*

*Corresponding author for this work

    Research output: Contribution to journalArticleAcademicpeer-review

    Abstract

    Preclinical drug testing in primary human cell models that recapitulate disease can significantly reduce animal experimentation and time-to-the-clinic. We used intestinal organoids to quantitatively study the potency of multivalent cholera toxin inhibitors. The method enabled the determination of IC50 values over a wide range of potencies (15 pM to 9 mM). The results indicate for the first time that an organoid-based swelling assay is a useful preclinical method to evaluate inhibitor potencies of drugs that target pathogen-derived toxins.

    Original languageEnglish
    Pages (from-to)6968-6972
    Number of pages5
    JournalJournal of Medicinal Chemistry
    Volume59
    Issue number14
    DOIs
    Publication statusPublished - 2016

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