Cloned (Comment) | Organism |
---|---|
expressed in Escherichia coli strain BL21 | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
unliganded PDE8A1 and in complex with 3-isobuytl-1-methylxanthine, hanging drop vapour diffusion method, using 100 mM sodium cacodylate (pH 6.5), 15% 2-propanol, 30% ethylene glycol, and 8-10% PEG3350 at 4°C | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
T748F | the mutation increases the PDE8A1 sensitivity to several nonselective or family selective PDE inhibitors, the catalytic efficiency of the mutant is about 2fold better than that of the wild type PDE8A1 | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-(6-aminopurin-9-yl)nonan-2-ol hydrochloride | - |
Homo sapiens | |
3-isobutyl-1-methylxanthine | nonselective inhibitor, the PDE8A1 catalytic domain is insensitive to 3-isobutyl-1-methylxanthine inhibition | Homo sapiens | |
BRL50481 | - |
Homo sapiens | |
dipyridamole | - |
Homo sapiens | |
etazolate | - |
Homo sapiens | |
MK298 | - |
Homo sapiens | |
papaverine | - |
Homo sapiens | |
rolipram | - |
Homo sapiens | |
sildenafil | - |
Homo sapiens | |
theophylline | weak inhibitor | Homo sapiens | |
zaprinast | - |
Homo sapiens | |
zardaverine | weak inhibitor | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0007 | - |
3',5'-cAMP | mutant enzyme T748A, in 20 mM Tris-HCl, pH 7.5, 4 mM MnCl2, at 24°C | Homo sapiens | |
0.0018 | - |
3',5'-cAMP | wild type PDE8A1 catalytic domain, in 20 mM Tris-HCl, pH 7.5, 4 mM MnCl2, at 24°C | Homo sapiens | |
1.6 | - |
3',5'-cGMP | wild type PDE8A1 catalytic domain, in 20 mM Tris-HCl, pH 7.5, 4 mM MnCl2, at 24°C | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O60658 | - |
- |
Purification (Comment) | Organism |
---|---|
Ni-NTA column chromatography | Homo sapiens |
Renatured (Comment) | Organism |
---|---|
refolding is initiated by addition of 0.03 mg/ml protein to a buffer of 0.5 M Tris-HCl pH 7.0, 20 mM MgCl2, 20 mM MnCl2, 0.020 mM ZnSO4, 0.7 M arginine, 30% glycerol, 10 mM NaCl, 1 mM KCl, and 10 mM dithiothreitol, at 4°C for three days | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
3',5'-cAMP + H2O | specific substrate | Homo sapiens | 5'-AMP | - |
? | |
3',5'-cGMP + H2O | low activity | Homo sapiens | 5'-GMP | - |
? |
Synonyms | Comment | Organism |
---|---|---|
cyclic nucleotide phosphodiesterase-8A | - |
Homo sapiens |
PDE8A | cAMP-specific enzyme | Homo sapiens |
PDE8A1 | PDE8A catalytic domain | Homo sapiens |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
1.6 | - |
3',5'-cGMP | wild type PDE8A1 catalytic domain, in 20 mM Tris-HCl, pH 7.5, 4 mM MnCl2, at 24°C | Homo sapiens | |
4 | - |
3',5'-cAMP | wild type PDE8A1 catalytic domain, in 20 mM Tris-HCl, pH 7.5, 4 mM MnCl2, at 24°C | Homo sapiens | |
4.3 | - |
3',5'-cAMP | mutant enzyme T748A, in 20 mM Tris-HCl, pH 7.5, 4 mM MnCl2, at 24°C | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0658 | - |
mutant enzyme T748A, in 20 mM Tris-HCl, pH 7.5, 4 mM MnCl2, at 24°C | Homo sapiens | 3-isobutyl-1-methylxanthine | |
0.698 | - |
wild type enzyme, in 20 mM Tris-HCl, pH 7.5, 4 mM MnCl2, at 24°C | Homo sapiens | 3-isobutyl-1-methylxanthine |