Functional Characterization of Cholera Toxin Inhibitors Using Human Intestinal Organoids.
Basic Information
ID: ALA4425128
Journal: J Med Chem
Title: Functional Characterization of Cholera Toxin Inhibitors Using Human Intestinal Organoids.
Authors: Zomer-van Ommen DD, Pukin AV, Fu O, Quarles van Ufford LH, Janssens HM, Beekman JM, Pieters RJ.
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.
CiteXplore: 27347611
DOI: 10.1021/acs.jmedchem.6b00770
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