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Cyclic GMP-specific phosphodiesterases are a superfamily of enzymes that hydrolyze 3',5'-cyclic guanosine monophosphate (cGMP) to 5'-GMP, thereby terminating cGMP signaling within cells. In mammals, these are encoded by several gene families (notably PDE5, PDE6, and PDE9), each with distinct tissue distributions, regulatory properties, and biological roles. These enzymes are molecular targets for important drugs, especially those treating erectile dysfunction and pulmonary hypertension, as well as emerging agents for heart failure and neurodegenerative diseases. Inhibitors of these enzymes prolong cGMP activity, resulting in beneficial effects such as vasodilation, improved cardiac function, or altered neuronal signaling, though their use requires attention to safety risks such as hypotension and drug interactions. It is essential to specify the isoform/family ("PDE5", "PDE6", etc.) to avoid ambiguity, since the term "cyclic GMP-phosphodiesterase" refers to a broad activity present in multiple proteins. If you need structured information on a particular isoform (e.g., "Phosphodiesterase 5A"), specify it for greater accuracy—this response covers the general target class based on your query.
Inhibition of cyclic GMP phosphodiesterase increases cGMP levels in target tissues, resulting in prolonged and amplified cGMP signaling. Effects include vasodilation, erection (smooth muscle relaxation), enhanced visual signal transmission (retina), and cardiac contractility modulation.
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