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For acquired resistance to AIs, we have developed an intratumoral aromatase breast cancer model to evaluate mechanisms of resistance to different AIs 12, 89. This model mimics hormone receptor-positive breast cancer in postmenopausal women. In our experiments, xenografts with tumors of MCF-7 cells overexpressing aromatase https://africahousingshow.com/kigtropin-200-iu-biotechnology-co-ltd/ (MCF-7Ca) were treated with letrozole and tumors were collected at different time points 90. We found that by 28 weeks after treatment, there was a significant decrease in total ERα expression. However, the levels of phosphorylated ERα (p-ERα) in letrozole-resistant tumors were significantly higher than p-ERα level at baseline.
It does this via three oxidation reactions of the androstenedione A ring, with each reaction consuming a molecule of both oxygen and NADPH per reaction. Of these three steps, the third is unique to aromatase, while the first two are common to P450 cytochrome proteins 19. Breast cancer tissues have been shown to express aromatase and produce higher levels of estrogens than non-cancerous cells.
Ask your doctor what other medications are better options for you. Arimidex may not be right for you if you have certain medical conditions or other factors that affect your health. Talk with your doctor about your health history before you take Arimidex. If your doctor confirms you had a serious allergic reaction to Arimidex, they may have you switch to a different treatment. For example, they may recommend taking an OTC pain reliever, such as acetaminophen or ibuprofen, to help ease this side effect. In some rare cases, side effects can result in permanent damage, even after you stop treatment with Arimidex.
The catalytic portion of cytochrome P450 aromatase contains a heme group as well as a steroid binding site 29. There are still several areas of aromatase function that are not thoroughly understood, such as the third aromatization step, as well as the underlying reason for its high substrate specificity. To address this, some investigators have utilized homology models of aromatase, based on other P450 enzyme structures 30.
For instance, some interactions can interfere with how well a drug works. Other interactions can increase the number of side effects or make them more severe. Researchers found that the 2.2% of women who took Aromasin had a complete response compared with 1.2% of women who took megestrol acetate. A partial response was seen in 12.8% of women who took Aromasin compared with 11.2% of women who took megestrol acetate. You should take Aromasin according to your doctor’s or healthcare provider’s instructions.