Green fluorescent protein-based halide indicators with improved chloride and iodide affinities.
AuthorsGalietta LJ, Haggie PM, Verkman AS,
JournalFEBS Lett
PubMed ID11423120
'The green fluorescent protein YFP-H148Q is sensitive to halides by a mechanism involving halide binding and a shift in pK(a). However, a limitation of YFP-H148Q is its low halide sensitivity, with K(d)>100 mM for Cl(-). Indicators with improved sensitivities are needed for cell transport studies, particularly in drug discovery by ... More
Restoration of chloride efflux by azithromycin in airway epithelial cells of cystic fibrosis patients.
AuthorsSaint-Criq V, Rebeyrol C, Ruffin M, Roque T, Guillot L, Jacquot J, Clement A, Tabary O,
JournalAntimicrob Agents Chemother
PubMed ID21220528
Azithromycin (AZM) has shown promising anti-inflammatory properties in chronic obstructive pulmonary diseases, and clinical studies have presented an improvement in the respiratory condition of cystic fibrosis (CF) patients. The aim of this study was to investigate, in human airway cells, the mechanism by which AZM has beneficial effects in CF. ... More
Small-molecule screen identifies inhibitors of a human intestinal calcium-activated chloride channel.
AuthorsDe La Fuente R, Namkung W, Mills A, Verkman AS,
JournalMol Pharmacol
PubMed ID18083779
Calcium-activated chloride channels (CaCCs) are widely expressed in mammalian tissues, including intestinal epithelia, where they facilitate fluid secretion. Potent, selective CaCC inhibitors have not been available. We established a high-throughput screen for identification of inhibitors of a human intestinal CaCC based on inhibition of ATP/carbachol-stimulated iodide influx in HT-29 cells ... More
Cell-based imaging of sodium iodide symporter activity with the yellow fluorescent protein variant YFP-H148Q/I152L.
The sodium iodide symporter (NIS) mediates iodide (I(-)) transport in the thyroid gland and other tissues and is of increasing importance as a therapeutic target and nuclear imaging reporter. NIS activity in vitro is currently measured with radiotracers and electrophysiological techniques. We report on the development of a novel live ... More