Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Blount, M.A.; Zoraghi, R.; Bessay, E.P.; Beasley, A.; Francis, S.H.; Corbin, J.D.
    Conversion of phosphodiesterase-5 (PDE5) catalytic site to higher affinity by PDE5 inhibitors (2007), J. Pharmacol. Exp. Ther., 323, 730-737.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
3.1.4.35 cGMP preincubation with cGMP increases catalytic activity for cGMP degradation, this increase may be caused by binding of cGMP to either the PDE5 allosteric sites, catalytic sites, or both. Full-length GAF-B subdomain conjoined with catalytic domain is sufficient for this conversion Bos taurus

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.1.4.35 expression in Sf9 system Bos taurus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.4.35 sildenafil preincubation with cGMP increases catalytic activity for cGMP degradation, but also for binding of inhibitor Bos taurus
3.1.4.35 tadalafil preincubation with cGMP increases catalytic activity for cGMP degradation, but also for binding of inhibitor Bos taurus
3.1.4.35 vardenafil preincubation with cGMP increases catalytic activity for cGMP degradation, but also for binding of inhibitor Bos taurus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.1.4.35 additional information Bos taurus preincubation with cGMP increases catalytic activity for cGMP degradation, thus elevated cellular cGMP initiates a physiological negative feedback on the cGMP pathway by increasing the affinity of the PDE5 catalytic site for cGMP ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.1.4.35 Bos taurus
-
 isoform PDE5
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.4.35 additional information preincubation with cGMP increases catalytic activity for cGMP degradation, thus elevated cellular cGMP initiates a physiological negative feedback on the cGMP pathway by increasing the affinity of the PDE5 catalytic site for cGMP Bos taurus ?
-
 ?