cGMP-dependent protein kinases in drug discovery
2005; Elsevier BV; Volume: 10; Issue: 9 Linguagem: Inglês
10.1016/s1359-6446(05)03406-9
ISSN1878-5832
AutoresJens Schlossmann, Franz Hofmann,
Tópico(s)Receptor Mechanisms and Signaling
ResumoCyclic guanosine-3', 5'-monophosphate (cGMP)-dependent protein kinases (cGKs) are key enzymes of nitric oxide-cGMP and natriuretic peptide signalling cascades. These kinases mediate most of the effects of cGMP-elevating drugs, such as nitrates and phosphodiesterase inhibitors. cGKs modulate smooth muscle relaxation (e.g. the vasculature, gastrointestinal tract, bladder and penile), platelet aggregation, renin release, intestinal secretion, learning and memory. Furthermore, several cGK substrates have been identified. Isozyme-specific inhibitors and activators of cGK and its downstream substrates might act more specifically than upstream signalling activators, such as organic nitrates and phosphodiesterase inhibitors.
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