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Literature summary for 3.1.4.53 extracted from

  • Wang, H.; Yan, Z.; Yang, S.; Cai, J.; Robinson, H.; Ke, H.
    Kinetic and structural studies of phosphodiesterase-8A and implication on the inhibitor selectivity (2008), Biochemistry, 47, 12760-12768.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.4.53

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli strain BL21 Homo sapiens

Crystallization (Commentary)

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

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

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 [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

Organism UniProt Comment Textmining
Homo sapiens O60658
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni-NTA column chromatography Homo sapiens

Renatured (Commentary)

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 and Products (Substrate)

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

Synonyms Comment Organism
cyclic nucleotide phosphodiesterase-8A
-
 Homo sapiens
PDE8A cAMP-specific enzyme Homo sapiens
PDE8A1 PDE8A catalytic domain Homo sapiens

Turnover Number [1/s]

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 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