Abstract
The cystic fibrosis transmembrane conductance regulator (CFTR) is a membrane protein that belongs to the same family as multidrug resistance-associated proteins whose main function is to expel xenobiotics and physiological organic anions from the cell interior. Despite the overall structural similarity with these membrane proteins, CFTR is not an active transporter but is instead a Cl- channel. We have tested the ability of known inhibitors of multidrug resistance-associated proteins to affect CFTR Cl- currents. We have found that sulfinpyrazone, probenecid, and benzbromarone are also inhibitors of CFTR activity, with a mechanism involving blockage of the channel pore.
| Original language | English |
|---|---|
| Pages (from-to) | 127-131 |
| Number of pages | 5 |
| Journal | European Journal of Pharmacology |
| Volume | 560 |
| Issue number | 2-3 |
| DOIs | |
| Publication status | Published - Apr 10 2007 |
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Keywords
- CFTR
- Channel blocker
- Chloride channel
- Multidrug resistance protein
ASJC Scopus subject areas
- Cellular and Molecular Neuroscience
- Pharmacology
Cite this
Block of CFTR-dependent chloride currents by inhibitors of multidrug resistance-associated proteins. / Diena, Tullia; Melani, Raffaella; Caci, Emanuela; Pedemonte, Nicoletta; Sondo, Elvira; Zegarra-Moran, Olga; Galietta, Luis J V.
In: European Journal of Pharmacology, Vol. 560, No. 2-3, 10.04.2007, p. 127-131.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Block of CFTR-dependent chloride currents by inhibitors of multidrug resistance-associated proteins
AU - Diena, Tullia
AU - Melani, Raffaella
AU - Caci, Emanuela
AU - Pedemonte, Nicoletta
AU - Sondo, Elvira
AU - Zegarra-Moran, Olga
AU - Galietta, Luis J V
PY - 2007/4/10
Y1 - 2007/4/10
N2 - The cystic fibrosis transmembrane conductance regulator (CFTR) is a membrane protein that belongs to the same family as multidrug resistance-associated proteins whose main function is to expel xenobiotics and physiological organic anions from the cell interior. Despite the overall structural similarity with these membrane proteins, CFTR is not an active transporter but is instead a Cl- channel. We have tested the ability of known inhibitors of multidrug resistance-associated proteins to affect CFTR Cl- currents. We have found that sulfinpyrazone, probenecid, and benzbromarone are also inhibitors of CFTR activity, with a mechanism involving blockage of the channel pore.
AB - The cystic fibrosis transmembrane conductance regulator (CFTR) is a membrane protein that belongs to the same family as multidrug resistance-associated proteins whose main function is to expel xenobiotics and physiological organic anions from the cell interior. Despite the overall structural similarity with these membrane proteins, CFTR is not an active transporter but is instead a Cl- channel. We have tested the ability of known inhibitors of multidrug resistance-associated proteins to affect CFTR Cl- currents. We have found that sulfinpyrazone, probenecid, and benzbromarone are also inhibitors of CFTR activity, with a mechanism involving blockage of the channel pore.
KW - CFTR
KW - Channel blocker
KW - Chloride channel
KW - Multidrug resistance protein
UR - http://www.scopus.com/inward/record.url?scp=33847411381&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=33847411381&partnerID=8YFLogxK
U2 - 10.1016/j.ejphar.2007.01.051
DO - 10.1016/j.ejphar.2007.01.051
M3 - Article
C2 - 17320853
AN - SCOPUS:33847411381
VL - 560
SP - 127
EP - 131
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
SN - 0014-2999
IS - 2-3
ER -