Neutral mutations to three acidic AF2 residues in the mouse estrogen receptor confer agonist activity to A-ring isomers of estradiol.

Abstract excerpt

The ability of the estrogen receptor (ER) to function as a ligand-mediated transcription factor involves the activation function-2 (AF2) in the hormone binding domain (HBD). Although several types of ligand bind to the ER, AF2 functions selectively, as it is activated by estradiol (E2) but not by antiestrogens. The mechanism used by AF2 to interpret the chemical and structural information encoded in the bound...

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