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Revisiting CFTR inhibition: a comparative study of CFTRinh -172 and GlyH-101 inhibitors.

Melis N, Tauc M, Cougnon M, Bendahhou S, Giuliano S, Rubera I, Duranton C - Br. J. Pharmacol. (2014)

Bottom Line: We also explored the effect of both inhibitors on cell viability using live/dead and cell proliferation assays in two different cell lines.The CFTRinh -172 did not affect the CaCC but did inhibit the VSORC, at concentrations higher than 5 µM.Our results provided insights into their use in mouse models.

View Article: PubMed Central - PubMed

Affiliation: University of Nice-Sophia Antipolis, LP2M CNRS-UMR7370, Faculté de médecine, Nice, France.

No MeSH data available.


Related in: MedlinePlus

Schematic representation of the specificity of CFTRinh-172 and GlyH-101 towards Cl− conductances, depending on the concentration used.
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fig06: Schematic representation of the specificity of CFTRinh-172 and GlyH-101 towards Cl− conductances, depending on the concentration used.

Mentions: Concerning CFTRinh-172, we noted that a concentration of 5 µM induced a full inhibition of the CFTR conductance along with no noticeable inhibition of the CaCC [as previously observed (Caputo et al., 2008) ] but a noticeable, but moderate, inhibition (from ∼15 to 50% depending on the cell type) of the VSORC. We conclude that, low concentrations of CFTRinh-172 (<10 µM) might represent the best experimental condition to provide fully inhibition of the CFTR conductance, with minimum effects on other Cl− conductances. Figure 6 summarises the concentration ranges of CFTRinh-172 and GlyH-101 used by us and their corresponding effects on CFTR, VSORC and CaCC conductances, expressed in mouse kidney epithelial cells.


Revisiting CFTR inhibition: a comparative study of CFTRinh -172 and GlyH-101 inhibitors.

Melis N, Tauc M, Cougnon M, Bendahhou S, Giuliano S, Rubera I, Duranton C - Br. J. Pharmacol. (2014)

Schematic representation of the specificity of CFTRinh-172 and GlyH-101 towards Cl− conductances, depending on the concentration used.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4128068&req=5

fig06: Schematic representation of the specificity of CFTRinh-172 and GlyH-101 towards Cl− conductances, depending on the concentration used.
Mentions: Concerning CFTRinh-172, we noted that a concentration of 5 µM induced a full inhibition of the CFTR conductance along with no noticeable inhibition of the CaCC [as previously observed (Caputo et al., 2008) ] but a noticeable, but moderate, inhibition (from ∼15 to 50% depending on the cell type) of the VSORC. We conclude that, low concentrations of CFTRinh-172 (<10 µM) might represent the best experimental condition to provide fully inhibition of the CFTR conductance, with minimum effects on other Cl− conductances. Figure 6 summarises the concentration ranges of CFTRinh-172 and GlyH-101 used by us and their corresponding effects on CFTR, VSORC and CaCC conductances, expressed in mouse kidney epithelial cells.

Bottom Line: We also explored the effect of both inhibitors on cell viability using live/dead and cell proliferation assays in two different cell lines.The CFTRinh -172 did not affect the CaCC but did inhibit the VSORC, at concentrations higher than 5 µM.Our results provided insights into their use in mouse models.

View Article: PubMed Central - PubMed

Affiliation: University of Nice-Sophia Antipolis, LP2M CNRS-UMR7370, Faculté de médecine, Nice, France.

No MeSH data available.


Related in: MedlinePlus