Altered Ligand Binding Properties and Enhanced Stability of a Constitutively Active Estrogen Receptor:  Evidence That an Open Pocket Conformation Is Required for Ligand Interaction

Abstract excerpt

To elucidate the ligand binding properties of the estrogen receptor (ER) and how ligand access to and release from the ligand binding pocket is affected by the conformational state of the receptor, we have measured the rates of estradiol association and dissociation, the equilibrium binding, and the stability of estradiol binding to denaturants, comparing wild-type human ER and a point mutant (Y537S ER) that...

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