| Literature DB >> 27347611 |
Domenique D Zomer-van Ommen1, Aliaksei V Pukin2, Ou Fu2, Linda H C Quarles van Ufford2, Hettie M Janssens3, Jeffrey M Beekman1, Roland J Pieters2.
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.Entities:
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Year: 2016 PMID: 27347611 DOI: 10.1021/acs.jmedchem.6b00770
Source DB: PubMed Journal: J Med Chem ISSN: 0022-2623 Impact factor: 7.446