Article
A ligand-mediated hydrogen bond network required for the activation of the mineralocorticoid receptor.
The Journal of biological chemistry - 2 Sept 2005
Bledsoe Randy K, Madauss Kevin P, Holt Jason A, Apolito Christopher J, Lambert Millard H, Pearce Kenneth H, Stanley Thomas B, Stewart Eugene L, Trump Ryan P, Willson Timothy M, Williams Shawn P
Abstract excerpt
Ligand binding is the first step in hormone regulation of mineralocorticoid receptor (MR) activity. Here, we report multiple crystal structures of MR (NR3C2) bound to both agonist and antagonists. These structures combined with mutagenesis studies reveal that maximal receptor activation involves an intricate ligand-mediated hydrogen bond network with Asn770 which serves dual roles: stabilization of the loop...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.