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Literature summary extracted from
- N-terminal domain of phosphodiesterase-11A4 (PDE11A4) decreases affinity of the catalytic site for substrates and tadalafil, and is involved in oligomerization (2007), Biochemistry, 46, 10353-10364.
Protein Variants
| EC Number | Protein Variants | Comment | Organism |
|---|---|---|---|
| 3.1.4.17 | additional information | the isolated PDE11 catalytic domain with residues M563-N934 displays both monomeric and dimeric forms. Isoforms containing at least 123 C-terminal amino acids of the GAF-B domain are stable oligomers, while the GAF-A domain is not required for oligomerization | Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.1.4.17 | tadalafil | - |
Homo sapiens |  |
| 3.1.4.17 | vardenafil | - |
Homo sapiens | |
KM Value [mM]
| EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 3.1.4.17 | 0.34 | - |
cGMP | isoform PDE11A2 | Homo sapiens | |
| 3.1.4.17 | 0.4 | - |
cGMP | isoform PDE11A1 | Homo sapiens | |
| 3.1.4.17 | 0.45 | - |
cAMP | isoform PDE11A1 | Homo sapiens | |
| 3.1.4.17 | 0.45 | - |
cAMP | isoform PDE11A2 | Homo sapiens | |
| 3.1.4.17 | 0.8 | - |
cAMP | isoform PDE11A3 | Homo sapiens | |
| 3.1.4.17 | 0.8 | - |
cGMP | isoform PDE11A3 | Homo sapiens | |
| 3.1.4.17 | 1 | - |
cGMP | isoform PDE11A4 | Homo sapiens | |
| 3.1.4.17 | 1.6 | - |
cAMP | isoform PDE11A4 | Homo sapiens | |
Molecular Weight [Da]
| EC Number | Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|---|
| 3.1.4.17 | 55000 | - |
2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1 | Homo sapiens |
| 3.1.4.17 | 56000 | - |
2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1 | Homo sapiens |
| 3.1.4.17 | 64000 | - |
2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1 | Homo sapiens |
| 3.1.4.17 | 66000 | - |
2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1 | Homo sapiens |
| 3.1.4.17 | 75000 | - |
2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1 | Homo sapiens |
| 3.1.4.17 | 78000 | - |
2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1 | Homo sapiens |
| 3.1.4.17 | 100000 | - |
2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1 | Homo sapiens |
| 3.1.4.17 | 105000 | - |
2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1 | Homo sapiens |
| 3.1.4.17 | 110000 | - |
isoform PDE11A2, gel filtration | Homo sapiens |
| 3.1.4.17 | 140000 | - |
isoform PDE11A3, gel filtration | Homo sapiens |
| 3.1.4.17 | 190000 | - |
isoform PDE11A4, gel filtration | Homo sapiens |
| 3.1.4.17 | 220000 | - |
isoform PDE11A1, gel filtration | Homo sapiens |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.1.4.17 | Homo sapiens | - |
splice variants A1, A2, A3, A4 of isoform PDE11 | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.1.4.17 | 3',5'-cAMP + H2O | - |
Homo sapiens | 5'-AMP | - |
? | |
| 3.1.4.17 | 3',5'-cGMP + H2O | - |
Homo sapiens | 5'-GMP | - |
? | |
| 3.1.4.17 | additional information | splice variants PDE11A1 and PDE11A2 show higher affinity for cAMP and cGMP than PDE11A4 | Homo sapiens | ? | - |
? | |
Subunits
| EC Number | Subunits | Comment | Organism |
|---|---|---|---|
| 3.1.4.17 | dimer | 2 * 105000, calculated, 2 * 100000, SDS-PAGE of PDE11A4, 2 * 78000, calculated, 2 * 75000, SDS-PAGE of PDE11A3, 2 * 66000, calculated, 2 * 64000, SDS-PAGE of PDE11A2, 2 * 56000, calculated, 2 * 55000, SDS-PAGE ofPDE11A1 | Homo sapiens |
IC50 Value
| EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|---|
| 3.1.4.17 | 0.000015 | - |
isoform PDE11A1 | Homo sapiens | tadalafil | |
| 3.1.4.17 | 0.000019 | - |
isoform PDE11A3 | Homo sapiens | tadalafil | |
| 3.1.4.17 | 0.000021 | - |
isoform PDE11A2 | Homo sapiens | tadalafil | |
| 3.1.4.17 | 0.000073 | - |
isoform PDE11A4 | Homo sapiens | tadalafil | |
| 3.1.4.17 | 0.000151 | - |
isoform PDE11A3 | Homo sapiens | vardenafil | |
| 3.1.4.17 | 0.000163 | - |
isoform PDE11A1 | Homo sapiens | vardenafil | |
| 3.1.4.17 | 0.000166 | - |
isoform PDE11A2 | Homo sapiens | vardenafil | |
| 3.1.4.17 | 0.00065 | - |
isoform PDE11A4 | Homo sapiens | vardenafil | |
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