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Literature summary 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

Cloned(Commentary)

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

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.1.4.53 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

EC Number Protein Variants Comment Organism
3.1.4.53 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

EC Number Inhibitors Comment Organism Structure
3.1.4.53 3-(6-aminopurin-9-yl)nonan-2-ol hydrochloride
-
 Homo sapiens
3.1.4.53 3-isobutyl-1-methylxanthine nonselective inhibitor, the PDE8A1 catalytic domain is insensitive to 3-isobutyl-1-methylxanthine inhibition Homo sapiens
3.1.4.53 BRL50481
-
 Homo sapiens
3.1.4.53 dipyridamole
-
 Homo sapiens
3.1.4.53 etazolate
-
 Homo sapiens
3.1.4.53 MK298
-
 Homo sapiens
3.1.4.53 papaverine
-
 Homo sapiens
3.1.4.53 rolipram
-
 Homo sapiens
3.1.4.53 sildenafil
-
 Homo sapiens
3.1.4.53 theophylline weak inhibitor Homo sapiens
3.1.4.53 zaprinast
-
 Homo sapiens
3.1.4.53 zardaverine weak inhibitor Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.1.4.53 0.0007
-
 3',5'-cAMP mutant enzyme T748A, in 20 mM Tris-HCl, pH 7.5, 4 mM MnCl2, at 24°C Homo sapiens
3.1.4.53 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
3.1.4.53 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

EC Number Organism UniProt Comment Textmining
3.1.4.53 Homo sapiens O60658
-
-

Purification (Commentary)

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

Renatured (Commentary)

EC Number Renatured (Comment) Organism
3.1.4.53 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)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.4.53 3',5'-cAMP + H2O specific substrate Homo sapiens 5'-AMP
-
 ?
3.1.4.53 3',5'-cGMP + H2O low activity Homo sapiens 5'-GMP
-
 ?

Synonyms

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

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.1.4.53 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
3.1.4.53 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
3.1.4.53 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

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.4.53 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
3.1.4.53 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