Mutation of R177 to Ala, Met, or Gln leads to increased basal kinase activity.
A, molecular model of inactive PKG1α showing putative packing of PKGα R177 in an inactive conformation. B, in silico-predicted destabilizing effects of mutations at R177 using the DUET server (ΔΔG in kcal/mol). C, kinase assays comparing basal to maximum cGMP-stimulated activation of WT and mutant PKG1α. Data are from triplicate reactions from a single protein preparation. The experiment was performed twice with similar results.