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Literature summary for 3.1.4.35 extracted from

  • Rybalkina, I.G.; Tang, X.B.; Rybalkin, S.D.
    Multiple affinity states of cGMP-specific phosphodiesterase for sildenafil inhibition defined by cGMP-dependent and cGMP-independent mechanisms (2010), Mol. Pharmacol., 77, 670-677.
    View publication on PubMed
Search for more literature for 3.1.4.35

Activating Compound

Activating Compound Comment Organism Structure
cGMP cGMP binding to the GAF-A domain is necessary to achieve full activation of PDE5, 3fold activation of blood platelet PDE5 occurs at 0.02 mM cGMP Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
sildenafil high sensitivity of PDE5 for sildenafil can be obtained through cGMP-induced activation of PDE or through cGMP-independent modulation of PDE5 in the nonactivated state Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3',5'-cGMP + H2O Homo sapiens
-
 5'-GMP
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
aortic smooth muscle cell
-
 Homo sapiens
-
blood platelet high expression of PDE5 in blood platelets Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3',5'-cGMP + H2O
-
 Homo sapiens 5'-GMP
-
 ?

Synonyms

Synonyms Comment Organism
cGMP-specific phosphodiesterase
-
 Homo sapiens
PDE5
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000016
-
 non-activated PDE5 from blood platelets, at 0.0001 mM cGMP, at pH 7.5 and 30°C Homo sapiens sildenafil
0.000005
-
 cGMP-activated PDE5 from blood platelets, at 0.0001 mM cGMP, at pH 7.5 and 30°C Homo sapiens sildenafil