GR-11-1 is a GRK2 substrate for phosphorylation. GR-11-1 exhibits lower sensitivity and affinity for G protein-coupled receptor kinase 2 [1].
In Vitro, GR-11-1 (50 μM; 60 min at 30 °C) functions as a substrate for recombinant human GRK2 (expressed in insect cells) with a Km of 33.9 μM and a Vmax of 0.35 pmol/min/mg, and exhibits low phosphorylation by recombinant human GRK5[1].
References:
[1]. Asai D, et al. A high-affinity peptide substrate for G protein-coupled receptor kinase 2 (GRK2). Amino Acids. 2019;51(6):973-976.
In Vitro, GR-11-1 (50 μM; 60 min at 30 °C) functions as a substrate for recombinant human GRK2 (expressed in insect cells) with a Km of 33.9 μM and a Vmax of 0.35 pmol/min/mg, and exhibits low phosphorylation by recombinant human GRK5[1].
References:
[1]. Asai D, et al. A high-affinity peptide substrate for G protein-coupled receptor kinase 2 (GRK2). Amino Acids. 2019;51(6):973-976.