Tamoxifen and raloxifene are the most widely prescribed selective estrogen receptor modulator (SERM) drugs used to treat breast cancer and prevent osteoporosis. Interactions between SERMs and mammalian cell membranes may control drug bioavailability and contribute to the drugs' anticancer actions, but are not well understood. To describe drug-membrane interactions with molecular detail, we investigated interfacial binding properties of raloxifene, tamoxifen and three tamoxifen metabolites (4-hydroxytamoxifen, N-desmethyltamoxifen and endoxifen) to planar supported lipid bilayers. The effects of lipid phase and order, cholesterol content, and drug charge on binding are quantified. Comparisons of SERM binding in the presence and absence of a peripheral estrogen receptor, ERa, incorporated in the lipid bilayer are also made.

Characterizing the interactions between planar supported lipid bilayers and selective estrogen receptor modulators (SERMs) using second harmonic generation spectroscopy

246th National Meeting (2013)

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