ArticleThe Journal of biological chemistry1998
Direct activation of cystic fibrosis transmembrane conductance regulator channels by 8-cyclopentyl-1,3-dipropylxanthine (CPX) and 1,3-diallyl-8-cyclohexylxanthine (DAX).
Article in The Journal of biological chemistry, 1998. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
17 citing papers in PubMed, 73 citations in OpenAlex.
- CFTR pharmacology.Cellular and molecular life sciences : CMLS · 2017Review
- Evaluation of Serum Adenosine Deaminase in Cystic Fibrosis Patients in an Iranian Referral Hospital.Iranian journal of pediatrics · 2016Article
- Article
- Monitoring charge flux to quantify unusual ligand-induced ion channel activity for use in biological nanopore-based sensors.Analytical chemistry · 2014Article
- Recent developments in adenosine receptor ligands and their potential as novel drugs.Biochimica et biophysica acta · 2011Review
- Introduction to adenosine receptors as therapeutic targets.Handbook of experimental pharmacology · 2009Review
- Amphiphilic pyridinium salts block TNF alpha/NF kappa B signaling and constitutive hypersecretion of interleukin-8 (IL-8) from cystic fibrosis lung epithelial cells.Biochemical pharmacology · 2005Article
- Reversal of cystic fibrosis phenotype in a cultured Delta508 cystic fibrosis transmembrane conductance regulator cell line by oligonucleotide insertion.Proceedings of the National Academy of Sciences of the United States of America · 2004Article
- Digitoxin mimics gene therapy with CFTR and suppresses hypersecretion of IL-8 from cystic fibrosis lung epithelial cells.Proceedings of the National Academy of Sciences of the United States of America · 2004Article
- Purinergic regulation of epithelial transport.The Journal of physiology · 2004Review
- Correction of G551D-CFTR transport defect in epithelial monolayers by genistein but not by CPX or MPB-07.British journal of pharmacology · 2002Article
- New therapeutic approaches for cystic fibrosis lung disease.Journal of the Royal Society of Medicine · 2002Review
- Pharmacogenomics of cystic fibrosis.Molecular interventions · 2001Review
- Pharmacogenomics of the cystic fibrosis transmembrane conductance regulator (CFTR) and the cystic fibrosis drug CPX using genome microarray analysis.Molecular medicine (Cambridge, Mass.) · 1999Article
- Update and Review: Cystic Fibrosis.Journal of genetic counseling · 1999Article
- Novel pharmacologic therapies for cystic fibrosis.The Journal of clinical investigation · 1999Review
- Regulation of murine cystic fibrosis transmembrane conductance regulator Cl- channels expressed in Chinese hamster ovary cells.The Journal of physiology · 1998Article
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
Abstract
8-Cyclopentyl-1,3-dipropylxanthine (CPX) and 1,3-diallyl-8-cyclohexylxanthine (DAX) are xanthine adenosine antagonists which activate chloride efflux from cells expressing either wild-type or mutant (DeltaF508) cystic fibrosis transmembrane conductance regulator (CFTR). These drugs are active in extremely low concentrations, suggesting their possible therapeutic uses in treating cystic fibrosis. However, knowledge of the mechanism of action of these compounds is lacking. We report here that the same low concentrations of both CPX and DAX which activate chloride currents from cells also generate a profound activation of CFTR channels incorporated into planar lipid bilayers. The process of activation involves a pronounced increase in the total conductive time of the incorporated CFTR channels. The mechanism involves an increase in the frequency and duration of channel opening events. Thus, activation by these drugs of chloride efflux in cells very likely involves direct interaction of the drugs with the CFTR protein. We anticipate that this new information will contribute fundamentally to the rational development of these and related compounds for cystic fibrosis therapy.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.