Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin–induced intestinal fluid secretion
Tonghui Ma, Jay R. Thiagarajah, Hong Yang, Nitin D. Sonawane, Chiara Folli, Luis J.V. Galietta, A.S. Verkman
Tonghui Ma, Jay R. Thiagarajah, Hong Yang, Nitin D. Sonawane, Chiara Folli, Luis J.V. Galietta, A.S. Verkman
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Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin–induced intestinal fluid secretion

Abstract

Research Article

Authors

Tonghui Ma, Jay R. Thiagarajah, Hong Yang, Nitin D. Sonawane, Chiara Folli, Luis J.V. Galietta, A.S. Verkman

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Characterization of CFTR inhibition by CFTRinh-172. (a) CFTR functional ...
Characterization of CFTR inhibition by CFTRinh-172. (a) CFTR functional assays as in Figure 1b for indicated [CFTRinh-172]. (b) Time course of inhibition showing CFTR-mediated I– transport rates at different times after addition of 2 μM CFTRinh-172. Inset: Time course of inhibition reversal showing I– transport rates at different times after washout of 1 μM CFTRinh-172. Mean ± SE is shown from three sets of experiments. (c) Inhibition of CFTR after stimulation by different agonists, including benzoflavone and benzimidazolone UCCF compounds (14), genistein, CPT-cAMP, 8-methoxypsoralen (8-MPO), and 8-cyclopentyl-1,3-dipropylxanthine (CPX) (all 50 μM) (SE; three sets of experiments). Black bars, agonist; white bars, agonist + 5 μM CFTRinh-172.