Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin–induced intestinal fluid secretion
Tonghui Ma, … , Luis J.V. Galietta, A.S. Verkman
Tonghui Ma, … , Luis J.V. Galietta, A.S. Verkman
Published December 1, 2002
Citation Information: J Clin Invest. 2002;110(11):1651-1658. https://doi.org/10.1172/JCI16112.
View: Text | PDF
Article

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

×

Figure 2

Options: View larger image (or click on image) Download as PowerPoint
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.