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Literature summary for 3.1.4.17 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
| Protein Variants | Comment | Organism |
|---|---|---|
| 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
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| tadalafil | - |
Homo sapiens |  |
| vardenafil | - |
Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.34 | - |
cGMP | isoform PDE11A2 | Homo sapiens | |
| 0.4 | - |
cGMP | isoform PDE11A1 | Homo sapiens | |
| 0.45 | - |
cAMP | isoform PDE11A1 | Homo sapiens | |
| 0.45 | - |
cAMP | isoform PDE11A2 | Homo sapiens | |
| 0.8 | - |
cAMP | isoform PDE11A3 | Homo sapiens | |
| 0.8 | - |
cGMP | isoform PDE11A3 | Homo sapiens | |
| 1 | - |
cGMP | isoform PDE11A4 | Homo sapiens | |
| 1.6 | - |
cAMP | isoform PDE11A4 | Homo sapiens | |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 110000 | - |
isoform PDE11A2, gel filtration | Homo sapiens |
| 140000 | - |
isoform PDE11A3, gel filtration | Homo sapiens |
| 190000 | - |
isoform PDE11A4, gel filtration | Homo sapiens |
| 220000 | - |
isoform PDE11A1, gel filtration | Homo sapiens |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
splice variants A1, A2, A3, A4 of isoform PDE11 | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 3',5'-cAMP + H2O | - |
Homo sapiens | 5'-AMP | - |
? | |
| 3',5'-cGMP + H2O | - |
Homo sapiens | 5'-GMP | - |
? | |
| additional information | splice variants PDE11A1 and PDE11A2 show higher affinity for cAMP and cGMP than PDE11A4 | Homo sapiens | ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| 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
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000015 | - |
isoform PDE11A1 | Homo sapiens | tadalafil | |
| 0.000019 | - |
isoform PDE11A3 | Homo sapiens | tadalafil | |
| 0.000021 | - |
isoform PDE11A2 | Homo sapiens | tadalafil | |
| 0.000073 | - |
isoform PDE11A4 | Homo sapiens | tadalafil | |
| 0.000151 | - |
isoform PDE11A3 | Homo sapiens | vardenafil | |
| 0.000163 | - |
isoform PDE11A1 | Homo sapiens | vardenafil | |
| 0.000166 | - |
isoform PDE11A2 | Homo sapiens | vardenafil | |
| 0.00065 | - |
isoform PDE11A4 | Homo sapiens | vardenafil | |
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