The goal of this project was to observe the effect of inhibitors of the sarco/endoplasmic reticulum calcium ATPase (SERCA) on calcium homeostasis in both healthy and cancerous human cell lines by fluorescence imaging. The SERCA inhibitors of interest were derivatives of hydroquinone and of bisphenol, whose in vitro inhibitory potencies had been determined previously in cell-free assays. Human skin fibroblasts and prostate cancer cells were grown in culture and loaded with a cell-permeant form of the fluorescent, calcium-sensitive dye Fura2, allowing the measurement of intracellular calcium concentrations with an imaging system. The experimental data showed that all inhibitors tested disrupted calcium homeostasis, which manifested itself by a sharp increase in intracellular calcium levels within approximately one minute after inhibitor application. This observation is compatible with the inhibition of SERCA in its native environment. It also suggests that the inhibitors can rapidly penetrate the cellular membrane and reach their target without being deactivated by intracellular enzymes.

Inhibition of the sacro/endoplasmic reticulum calcium ATPase in healthy and cancerous cell lines: A fluorescence calcium imaging study

246th National Meeting (2013)

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