Heiner Apeler

TL;DR: A pyrazolopyridine is presented that potently stimulates sGC through this site by a mechanism that is independent of NO, which results in antiplatelet activity, a strong decrease in blood pressure and an increase in survival in a low-NO rat model of hypertension, and may offer an approach for treating cardiovascular diseases.

TL;DR: A novel type of sGC activator which activates the enzyme even after it has been oxidized by the sGC inhibitor ODQ or rendered haem deficient is identified and may offer a new approach for treating cardiovascular diseases.

TL;DR: The expression/purification procedure is suitable for producing large amounts of highly pure sGC which contains one heme per heterodimer without a reconstitution step and the activator experiments show that in a synergistic stimulation with YC-1 sGC can be activated maximally both by nitric oxide and by carbon monoxide and that Yc-1 does not directly act via heme.

TL;DR: The results suggest that BAY 41‐8543 is on the one hand an invaluable tool for studying sGC signaling in vitro and on the other hand its unique profile may offer a novel approach for treating cardiovascular diseases.

TL;DR: The data demonstrate that the region surrounding the cysteines 238 and 243 in the α1-subunit of the sGC could play an important role in regulation of s GC activity and could be the target of this new type of sGC stimulators.