Figure 5.

(A) Molecular model of candesartan (red), telmisartan (magenta) and eprosartan (blue) docking to AT₁ receptors. Comparison of the AT₁ receptor binding pocket interactions with (B) candesartan, (C) telmisartan and (D) eprosartan in the ground state (WT‐AT₁ receptor) and active state (N111G‐AT₁ receptor). The ARBs are shown as sticks with red (candesartan), magenta (telmisartan) and blue (eprosartan) carbons. Side‐chain positions of residues investigated in this report are located within a 10 Å pocket for each ARB. In each ARB‐bound model, single side‐chain mutations affecting binding with a >3‐fold change in K_i are indicated by a thick green colour and bold label, both in the ground state (WT‐AT₁ receptor) and active state (N111G‐AT₁ receptor). A red residue label denotes a significant effect on inverse agonism for IP formation in WT‐ and N111G‐AT₁ receptors. Highlighted residues shown as yellow spheres denote a unique influence on inverse agonism for IP formation in the specified state of AT₁ receptors for the particular ARB.