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Regulation of gene expression by sequence-specific DNA binding proteins involves the co-ordinated action of a repertoire of transcriptional coregulator complexes, which together act to modify chromatin at gene promoters, thereby facilitating gene expression. The mechanisms by which such coregulators are recruited to the promoters of estrogen-responsive genes by estrogen receptor-\upalpha have been well studied in breast cancer cells. These studies have highlighted coactivator and corepressor proteins that appear to be critical for the agonist and antagonist actions of estrogen and anti-estrogens, and indicate that altered levels and/or activities of these proteins is an important feature of response and resistance to endocrine treatments in breast cancer.