Article
Tyrosine-612 in PDE5 contributes to higher affinity for vardenafil over sildenafil.
International journal of impotence research - 1 Jan 2000
Corbin J, Francis S, Zoraghi R
Abstract excerpt
Despite close structural similarity, vardenafil (Levitra) is 32-fold more potent than sildenafil (Viagra) to inhibit cGMP-binding cGMP-specific PDE (PDE5); this is due to differences between their heterocyclic rings. In co-crystals with PDE5, one of the rings of vardenafil or sildenafil interacts with Tyr(612), a catalytic site AA, via (1) a hydrogen bond with a water molecule and (2) hydrophobic bonds. For...
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