Multiple Conformations of Phosphodiesterase-5

Multiple conformations of phosphodiesterase-5: implications for enzyme function and drug development.

Phosphodiesterase-5 (PDE5) is the target for sildenafil, vardenafil, and tadalafil, which are drugs for treatment of erectile dysfunction and pulmonary hypertension. We report here the crystal structures of a fully active catalytic domain of unliganded PDE5A1 and its complexes with sildenafil or icarisid II. These structures together with the PDE5A1-isobutyl-1-methylxanthine complex show that t...

Evolution of Phosphodiesterase-5 Inhibitors.

Correspondence to: Du Geon Moon Department of Urology, Korea University Guro Hospital, 148 Gurodong-ro, Guro-gu, Seoul 08308, Korea. Tel: +82-2-2626-3201, Fax: +82-2-2626-1321, E-mail: [email protected] Copyright © 2015 Korean Society for Sexual Medicine and Andrology This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://c...

Pulmonary responses to selective phosphodiesterase-5 and phosphodiesterase-3 inhibitors.

OBJECTIVE To compare the direct pulmonary vasodilating activity and specificity of phosphodiesterase-5 (zaprinast) and phosphodiesterase-3 (milrinone) inhibitors on the pulmonary vascular (PV) bed of the spontaneously breathing cat with an intact chest. DESIGN Prospective, randomized animal study. SETTING Laboratory of university hospital. SUBJECTS Experiments were performed in vivo in in...

AB030. Evolution of phosphodiesterase type 5 inhibitors

After launching of sildenafil citrate, the last invention of 20 century, in 1998, oral phosphodiesterase type 5 (PDE5) inhibitor has been established as first line treatment of erectile dysfunction and shift new paradigm of diagnosis and treatment of erectile dysfunction. The big success of sildenafil in pharmaceutical R&D induced the consecutive development of the so-called ‘The second Viagra’...

Anti-cancer Role of Phosphodiesterase-5 Inhibitors