The PI-PLC inhibitor U-73122 is a potent inhibitor of the SERCA pump in smooth muscle.
In this issue MacMillan and McCarron in 2010 demonstrated that the phospholipase C (PLC) inhibitor U-73122 can potently inhibit Ca(2+) release from isolated smooth muscle cells independent of its effect on PLC. Their data suggest that the PLC inhibitor can block the sarcoplasmic/endoplasmic reticulum calcium ATPase pump in smooth muscle and cast doubt on the reliability of U-73122 as the main pharmacological tool to assess the role of the phosphotidyl inositol-PLC pathway in cellular signalling.
Hollywood
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MA
Smooth Muscle Research Centre, Dundalk Institute of Technology, Co. Louth, Ireland. mark.hollywood@dkit.ie
Sergeant
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GP
Thornbury
K D
KD
McHale
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NG
D000818:Animals; D002118:Calcium / Q000378:metabolism; D004963:Estrenes / Q000494:pharmacology*; D006801:Humans; D032389:Myocytes, Smooth Muscle / Q000187:drug effects / Q000378:metabolism; D054801:Phosphoinositide Phospholipase C / Q000037:antagonists & inhibitors*; D011760:Pyrrolidinones / Q000494:pharmacology*; D053498:Sarcoplasmic Reticulum Calcium-Transporting ATPases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015398:Signal Transduction
D004963:Estrenes; D011760:Pyrrolidinones; C060229:1-(6-((3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione; D054801:Phosphoinositide Phospholipase C; D053498:Sarcoplasmic Reticulum Calcium-Transporting ATPases; D002118:Calcium