Fig. 3: Structural comparison between active and inactive α1AAR.
From: Structural basis of α1A-adrenergic receptor activation and recognition by an extracellular nanobody
a Comparison of α1AAR between oxymetazoline-bound (blue), noradrenaline-bound (green), and inactive (orange) states viewed from the side. b Intracellular view of superposed α1AARs. Distances were measured between the Cα atoms of E2696.30 (E269L6.30 in α1AAR-kOR) in TM6, K2125.66 in TM5, and C3287.55 in TM7. c Extracellular view of superposed α1AARs. The maximum distances of the side chain displacement of W285 (position 7th carbon of the indole ring) are 2.4 Å between the noradrenaline-bound active state and the tamsulosin-bound inactive state, and 1.8 Å between the oxymetazoline-bound state and the tamsulosin-bound state. d Conformational change of PIF motif and toggle switch W2856.48. e Conformational change of DRY and NpxxY motifs. Conformational changes upon activation are shown with magenta arrows. Hydrogen bonds are shown as black dashed lines.
