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G protein-coupled receptor kinase 2 (GRK2) phosphorylates activated G protein-coupled receptors (GPCRs), which ultimately leads to their desensitization and/or downregulation. The enzyme is recruited to the plasma membrane via the interaction of its carboxyl-terminal pleckstrin-homology (PH) domain with the β and γ subunits of heterotrimeric G proteins (Gβγ). An improved purification scheme for GRK2 has been developed, conditions under which GRK2 forms a complex with Gβ1γ2 have been determined and the complex has been crystallized in CHAPS detergent micelles. Crystals of the GRK2–Gβγ complex belong to space group C2 and have unit-cell parameters a = 187.0, b = 72.1, c = 122.0 Å, β = 115.2°. A complete data set has been collected to 3.2 Å resolution with Cu Kα radiation.

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