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“ Tamoxifen inhibits transmembrane currents of the Kir2.x inward rectifier potassium channels by interfering with the interaction of the channels with membrane phosphatidylinositol 4,5-bisphosphate (PIP(2)).”
Journal of pharmacological sciences • 2010 | View Paper
“Pretreatment with PIP2 significantly decreased the inhibition induced by tamoxifen , 4-hydroxytamoxifen, and raloxifene on Kir2.3 channels.”
“We tested the hypothesis that tamoxifen interferes with the interaction between the channel and the membrane-delimited channel activator, phosphatidylinositol 4,5-bisphosphate (PIP2).”
Journal of Pharmacology and Experimental Therapeutics • 2009 | View Paper
“Our results suggest that tamoxifen inhibited Kv7.2/Kv7.3 channels by interfering with PIP2-channel interaction because of its documented interaction with PIP2 and the similar effect of tamoxifen on various PIP2 sensitive channels.”
“For members of the inward-rectifying K+ (Kir) channel family, interference of Tmx with binding of phosphatidylinositol 4,5-bisphosphate (PIP2) has been suggested as the mechanism underlying such inhibition.”