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Tamoxifen is a precursor for the drug that binds to the estrogen receptor, making it a prodrug. The actual drug is 4-hydroxyltamoxifen, which has a greater affinity for the estrogen receptor than Tamoxifen alone. The FDA approved this prodrug 30 years ago to prevent breast cancer in high risk patients. Tamoxifen is classfied as a Seletive Estrogen Receptor Modulator (SERM), meaning that it selectively blocks or activates the activity of estrogen on specific cells, such as breast cancer cells. While Tamoxifen is used to block estrogen acivity in breast cells, it also activates estrogen actrivity in other cells, such as bone and liver cells.
Tamoxifen is a precursor for the drug that binds to the estrogen receptor, making it a prodrug. The actual drug is 4-hydroxyltamoxifen, which has a greater affinity for the estrogen receptor than Tamoxifen alone. The FDA approved this prodrug 30 years ago to prevent breast cancer in high risk patients. Tamoxifen is classfied as a Seletive Estrogen Receptor Modulator (SERM), meaning that it selectively blocks or activates the activity of estrogen on specific cells, such as breast cancer cells. While Tamoxifen is used to block estrogen acivity in breast cells, it also activates estrogen actrivity in other cells, such as bone and liver cells.


[[Image:estrogen.PNG|Caption=The Drug Tamoxifen and the Tamoxifen-Estrogen Complex. The green area represents the change in signal loop due to conformational changes after ligand-binding of Tamoixfen|]]
[[Image:estrogen.PNG|Caption='The Drug Tamoxifen and the Tamoxifen-Estrogen Complex. The green area represents the change in signal loop due to conformational changes after ligand-binding of Tamoixfen'|]]

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA, Andrea Danielle Merr, John Means