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Therapeutic strategies to block estrogen receptor function: Aromatase inhibitors like letrozole, anastrozole and exemestane inhibit the enzyme leading to decreased E2 levels. Selective ER downregulators (SERDs) like fulvestrant bind to ER and sequester it, thereby inhibiting ER-mediated gene transcripton and disrupting ER nuclear localization through the ubiquitin-proteosomal pathway.
