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Literature summary for 3.1.4.35 extracted from

  • Reingruber, J.; Holcman, D.
    Estimating the rate constant of cyclic GMP hydrolysis by activated phosphodiesterase in photoreceptors (2008), J. Chem. Phys., 129, 145102.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
additional information phosphorylation acts in concert with allosteric cGMP binding to stimulate the PDE5 catalytic site, which should promote negative feedback regulation of the cGMP pathway in intact cells Homo sapiens
additional information phosphorylation acts in concert with allosteric cGMP binding to stimulate the PDE5 catalytic site, which should promote negative feedback regulation of the cGMP pathway in intact cells Bos taurus

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens
-
Bos taurus

Inhibitors

Inhibitors Comment Organism Structure
tadalafil cGMP modestly but significantly increases the affinity of PDE5 for tadalafil by 1.7fold Bos taurus
tadalafil cGMP modestly but significantly increases the affinity of PDE5 for tadalafil by 1.7fold Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0247
-
2'-O-anthraniloyl-cGMP phosphorylated PDE5, at 30°C with 50 mM Tris-HCl, pH 7.5 Homo sapiens
0.0651
-
2'-O-anthraniloyl-cGMP unphosphorylated PDE5, at 30°C with 50 mM Tris-HCl, pH 7.5 Homo sapiens

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
side-chain modification PDE5 is phosphorylated at Ser102 by cyclic nucleotide-dependent protein kinases, phosphorylation activates PDE5 catalytic site independently of cGMP binding to the allosteric sites Homo sapiens
side-chain modification PDE5 is phosphorylated at Ser92 by cyclic nucleotide-dependent protein kinases, phosphorylation activates PDE5 catalytic site independently of cGMP binding to the allosteric sites Bos taurus

Purification (Commentary)

Purification (Comment) Organism
Ni-NTA agarose column chromatography Homo sapiens
Ni-NTA agarose column chromatography Bos taurus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2'-O-anthraniloyl-cGMP + H2O phosphorylation increases affinity for hydrolysis of 2'-O-anthraniloyl-cGMP by about 3fold Homo sapiens ?
-
?
2'-O-anthraniloyl-cGMP + H2O phosphorylation increases affinity for hydrolysis of 2'-O-anthraniloyl-cGMP by about 3fold Bos taurus ?
-
?
3',5'-cGMP + H2O
-
Homo sapiens 5'-GMP
-
?
3',5'-cGMP + H2O
-
Bos taurus 5'-GMP
-
?
additional information tadalafil is not degraded by PDE5 Homo sapiens ?
-
?
additional information tadalafil is not degraded by PDE5 Bos taurus ?
-
?

Synonyms

Synonyms Comment Organism
PDE5
-
Homo sapiens
PDE5
-
Bos taurus
phosphodiesterase-5
-
Homo sapiens
phosphodiesterase-5
-
Bos taurus