Fig. 5: Cryo-EM structure of drug-bound rMrp2.
From: Structural basis for the modulation of MRP2 activity by phosphorylation and drugs
a Density for two probenecid molecules (shown in orange sticks) and one CHS molecule (shown in grey sticks) within the TMD; their structures are shown for reference. b Binding of probenecid displaces the R-___domain from the TMD. c The two probenecid molecules are coordinated by hydrogen bonds and π-stacking interactions within the TMD. Left panel is a view along the membrane and right panel is a view from the cytosol. d The probenecid bound structure defines the two drug binding sites that are in close proximity to each other.
