Steroidal and Non-steroidal Mineralocorticoid Receptor Antagonists in Cardiorenal Medicine

Rajiv Agarwal; Peter Kolkhof; George Bakris; Johann Bauersachs; Hermann Haller; Takashi Wada; Faiez Zannad


Eur Heart J. 2021;42(2):152-161. 

In This Article

Steroid Hormone Receptors and Their Ligands

Steroid hormone receptors comprise a subfamily of nuclear receptors that act as intracellular receptors and nuclear transcription factors. This subfamily consists of the androgen receptor, the glucocorticoid receptor (GR), the MR, the progesterone receptor, and oestrogen receptors. The GR is activated by cortisol, whereas the MR is promiscuous with the same binding affinity for aldosterone and cortisol.[4] MRs mediate fluid, electrolyte, and haemodynamic homeostasis, as well as tissue repair.[4] GR modulation impacts energy homeostasis, stress responses, and inflammation.[4] Because MRs and GRs are often expressed in the same tissues and cells, regulating their functional interactions is key to maintaining homeostatic balance.[4] Interestingly, progesterone also acts as an endogenous MRA because it can compete with aldosterone for MR binding with similar affinity.[4]