PKG drug G1 is an activator of protein kinase GIα (PKGIα).1 It induces relaxation in U-46619-precontracted mesenteric arteries isolated from wild-type, but not oxidation-insensitive Cys42Ser PKGIα knock-in, mice in a concentration-dependent manner. PKG drug G1 (14.8 mg/kg) induces oxidation of PKGIα, a marker of activation, in the aorta in a mouse model of angiotensin II-induced hypertension. It decreases mean arterial pressure in the same model when administered at a dose of 20 mg/kg per day for four days.
1.Burgoyne, J.R., Prysyazhna, O., Richards, D.A., et al.Proof of principle for a novel class of antihypertensives that target the oxidative activation of PKG Iα (protein kinase G Iα)Hypertension70(3)577-586(2017)