Figure 6

Figure 6

The substitution of the threonine 870 by a leucine increased the efficacy of steroids on hMR

Dose-response curves of (A) 17α-hydroxyprogesterone, medrol, progesterone, drospirenone, and spironolactone and (B) finerenone and eplerenone in UG5LN-GAL4-hMR (T870L) cells. 17α-hydroxyprogesterone, medrol, progesterone, drospirenone, and spironolactone were tested alone (agonism test).

(B) Finerenone and eplerenone were tested in the presence of aldosterone 0.5 10⁻⁹ M (antagonism test). Results are expressed as the percentage of the maximum luciferase activity induced by 10⁻⁸ M aldosterone. The curves are presented as a non-linear regression; log (ligand) versus response. EC₅₀ values (10⁻⁹ M) and IC₅₀ values (10⁻⁹ M) are shown in Tables 5 and 6.

Data are presented as means ± SD values. n (replicates per experiment) = 4 per group.