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J Med Chem. 2016 Jul 28;59(14):6968-72. doi: 10.1021/acs.jmedchem.6b00770. Epub 2016 Jul 7.

Functional Characterization of Cholera Toxin Inhibitors Using Human Intestinal Organoids.

Author information

1
Department of Pediatric Pulmonology, University Medical Centre Utrecht , Lundlaan 6, 3508 GA Utrecht, The Netherlands.
2
Department of Chemical Biology & Drug Discovery, Utrecht Institute for Pharmaceutical Sciences, Utrecht University , P.O. Box 80082, 3508 TB Utrecht, The Netherlands.
3
Department of Pediatric Pulmonology, Erasmus Medical Center/Sophia Children's Hospital , Wytemaweg 80, 3015 CN Rotterdam, The Netherlands.

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.

PMID:
27347611
DOI:
10.1021/acs.jmedchem.6b00770
[Indexed for MEDLINE]
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