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This selective molecular recognition pattern based on the distinct domains of GRK2 establishes a link between the open/closed conformational states of GRK2 and its selective interactions with different binding molecules and provides a structural basis for the elucidation of how different classes of inhibitors target these specific interaction interfaces, including the GRK2–Gαq interface, the GRK2–Gβγ interaction and the GRK2 KD–substrate interaction [1, 7]