Endocrine Abstracts

Sustained mineralocorticoid receptor (MR) signalling promotes cardiac inflammation and fibrosis, which ultimately leads to cardiac failure. While the clinical use of MR antagonists are protective in cardiac disease, hyperkaelemia, and other off target effects have limited their use. In order to identify key MR-dependent mechanisms of heart disease progression that are distinct to normal renal electrolyte control, we have developed a series of tissue selective MR null animal mo...

The mineralocorticoid receptor (MR) has a modular domain structure containing a C-terminal ligand-binding domain (LBD) that consists of 11 α-helices (designated H1 to H12) organized in an antiparallel helical sandwich. The LBD undergoes a conformational change upon aldosterone binding such that H12 forms a stable interaction with helices 3, 4 and 5 to create an AF-2 domain, a hydrophobic cleft on the surface of the LBD, which serves as a docking platform for transcription...