Molecular Basis of Sex Hormone Receptor Function New Targets for Intervention [Paperback]

How sex hormone receptors and all the other members of the nuclear receptor superfamily do such a remarkable job has fascinated scientists for decades. A series of discoveries in the past few years has dramatically enlightened our understanding of the molecular mechanisms that govern nuclear receptor action. The elucidation of the 3D structures of several nuclear receptor ligand binding domains in the presence of agonists or antagonists has provided an allosteric concept of ligand action, and the discovery of a plethora of ligand-dependent protein interactions has linked this transconformation with the ability of nuclear receptors to act as transcriptional activators and repressors and the enzymatic modification of chromatin and factors of the basal transcriptional machinery.How sex hormone receptors and all the other members of the nuclear receptor superfamily do such a remarkable job has fascinated scientists for decades. A series of discoveries in the past few years has dramatically enlightened our understanding of the molecular mechanisms that govern nuclear receptor action. The elucidation of the 3D structures of several nuclear receptor ligand binding domains in the presence of agonists or antagonists has provided an allosteric concept of ligand action, and the discovery of a plethora of ligand-dependent protein interactions has linked this transconformation with the ability of nuclear receptors to act as transcriptional activators and repressors and the enzymatic modification of chromatin and factors of the basal transcriptional machinery.From the contents:Nuclear Receptors as Targets for Drug Design: New Options and Old Challenges.- The Androgen Receptor Coregulator ARA70.- Role of Coactivators in Transcriptional Activation by Estrogen Receptors.- A Search for a Mechanism for the Antiinflammatory Action of Glucocorticoids.- Activation of Progesterone and Androgen Receptors by Signal Transduction Pathways.- Ligand-Independent Activation of the Estrogen Receptl+