Activation of nuclear receptors: a perspective from structural genomics.

  title={Activation of nuclear receptors: a perspective from structural genomics.},
  author={Yong Li and Millard H. Lambert and Hailou Xu},
  volume={11 7},
Crystal structures of more than two dozen different nuclear receptor ligand binding domains have defined a simple paradigm of receptor activation, in which agonist binding induces the activation function-2 (AF-2) helix to form a charge clamp for coactivator recruitment. Recent structural studies present a surprising contrast. Activation of the mouse LRH-1 receptor is independent of a bound agonist despite its large ligand binding pocket, whereas the activation of the Drosophila DHR38 receptor… CONTINUE READING

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