Fig. 1: Cryo-EM structures of V2R bound to tolvaptan and conivaptan.
From: Structural insights into antagonist recognition by the vasopressin V2 receptor
a Schematic illustration of the regulatory function of V2R by endogenous hormone arginine vasopressin (AVP) and the antagonists tolvaptan and conivaptan. b Optimized construct for the structure determination of antagonist-bound V2R. c, d Orthogonal views of the density maps (left panel) and the models (right panel) of tolvaptan-V2R-Fab (c) and conivaptan-V2R-Fab complex (d). Tolvaptan-bound V2R is in green, tolvaptan is in pink, conivaptan-bound V2R is in purple, conivaptan is in orange, Fab-LC is in dark blue, Fab-HC is in cyan, BRIL is in gray. Components of V2R complexes are colored as indicated, with the EM density maps for tolvaptan and conivaptan displayed as transparent surfaces at contour levels of 0.40 and 0.26, respectively. LC light chain, HC heavy chain.
