A quantitative description of the activation and inhibition of CFTR by potentiators: Genistein

Oscar Moran, Olga Zegarra-Moran

Research output: Contribution to journalArticlepeer-review

Abstract

The CFTR, encoded by the gene mutated in cystic fibrosis (CF) patients, is responsible for cAMP dependent chloride transport in epithelia. Substances that activate CFTR have been suggested as possible CF therapy. Most substances investigated so far exert a dual effect on the CFTR: low concentrations stimulate CFTR, whereas higher concentrations inhibit CFTR. Besides, the CFTR phosphorylation level determines the apparent affinity of the drug. We have studied the properties of genistein, the well known CFTR potentiator, by measuring apical membrane current on epithelia formed by cells stably transfected with CFTR and stimulated with different concentrations of CPTcAMP. We propose a quantitative model to describe the activatory and inhibitory effect of genistein, accounting also for the cAMP dependent activation.

Original languageEnglish
Pages (from-to)3979-3983
Number of pages5
JournalFEBS Letters
Volume579
Issue number18
DOIs
Publication statusPublished - Jul 18 2005

Keywords

  • Chloride transport
  • Cystic fibrosis
  • Nucleotide binding domain

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

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