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 (Comment) | Organism |
---|---|
- |
Homo sapiens |
- |
Bos taurus |
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 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 | UniProt | Comment | Textmining |
---|---|---|---|
Bos taurus | - |
- |
- |
Homo sapiens | - |
- |
- |
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 (Comment) | Organism |
---|---|
Ni-NTA agarose column chromatography | Homo sapiens |
Ni-NTA agarose column chromatography | Bos taurus |
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 | Comment | Organism |
---|---|---|
PDE5 | - |
Homo sapiens |
PDE5 | - |
Bos taurus |
phosphodiesterase-5 | - |
Homo sapiens |
phosphodiesterase-5 | - |
Bos taurus |