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- Domenique D Zomer-van Ommen, Aliaksei V Pukin, Ou Fu, Linda H C Quarles van Ufford, Hettie M Janssens, Jeffrey M Beekman, and Roland J Pieters.
- Department of Pediatric Pulmonology, University Medical Centre Utrecht , Lundlaan 6, 3508 GA Utrecht, The Netherlands.
- J. Med. Chem. 2016 Jul 28; 59 (14): 6968-72.
AbstractPreclinical 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.
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