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Literature summary extracted from

  • Barren, B.; Gakhar, L.; Muradov, H.; Boyd, K.K.; Ramaswamy, S.; Artemyev, N.O.
    Structural basis of phosphodiesterase 6 inhibition by the C-terminal region of the gamma-subunit (2009), EMBO J., 28, 3613-3622.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.1.4.35 chimaeric PDE5/PDE6 catalytic domain is expressed in Escherichia coli BL21-codon plus cells Bos taurus

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.1.4.35 chimaeric PDE5/PDE6 catalytic domain complexed with sildenafil or 3-isobutyl-1-methylxanthine and the Pgamma-inhibitory peptide Pgamma70-87, hanging drop vapor diffusion method, using 100 mM Tris (pH 8.5), 200 mM MgSO4, 12% (w/v) PEG-3350, and 2.5% (v/v) ethanol, at 4°C Bos taurus

Protein Variants

EC Number Protein Variants Comment Organism
3.1.4.35 N661A the substitution moderately increases the Km value for cGMP hydrolysis but it markedly decreases the potency of PDE5/6cd inhibition by Pgamma inhibitory peptide Bos taurus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.4.35 3-isobutyl-1-methylxanthine
-
 Bos taurus
3.1.4.35 Pgamma-inhibitory peptide
-
 Bos taurus
3.1.4.35 Pgamma-inhibitory peptide Pgamma63-87
-
 Bos taurus
3.1.4.35 Pgamma-inhibitory peptide Pgamma70-87
-
 Bos taurus
3.1.4.35 sildenafil
-
 Bos taurus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.1.4.35 0.0036
-
 3',5'-cGMP chimaeric PDE5/PDE6 catalytic domain, pH and temperature not specified in the publication Bos taurus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.1.4.35 3',5'-cGMP + H2O Bos taurus PDE5 and PDE6 show specificity for cGMP relative to cAMP 5'-GMP
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.1.4.35 Bos taurus
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.1.4.35 NiSO4-charged His-bind resin column chromatography and benzamidine Sepharose column chromatography Bos taurus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.4.35 3',5'-cGMP + H2O PDE5 and PDE6 show specificity for cGMP relative to cAMP Bos taurus 5'-GMP
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.4.35 PDE5
-
 Bos taurus
3.1.4.35 PDE5/PDE6cd chimaeric PDE5/6 catalytic domain Bos taurus
3.1.4.35 PDE6
-
 Bos taurus
3.1.4.35 phosphodiesterase-5
-
 Bos taurus
3.1.4.35 phosphodiesterase-6
-
 Bos taurus

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.1.4.35 0.55
-
 3',5'-cGMP chimaeric PDE5/PDE6 catalytic domain, pH and temperature not specified in the publication Bos taurus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.1.4.35 0.000025
-
 sildenafil chimaeric PDE5/6 catalytic domain, pH and temperature not specified in the publication Bos taurus
3.1.4.35 0.0015
-
 Pgamma-inhibitory peptide chimaeric PDE5/6 catalytic domain, pH and temperature not specified in the publication Bos taurus
3.1.4.35 0.0029
-
 Pgamma-inhibitory peptide Pgamma63-87 chimaeric PDE5/6 catalytic domain, pH and temperature not specified in the publication Bos taurus
3.1.4.35 0.0085
-
 3-isobutyl-1-methylxanthine chimaeric PDE5/6 catalytic domain, pH and temperature not specified in the publication Bos taurus
3.1.4.35 0.0121
-
 Pgamma-inhibitory peptide Pgamma70-87 chimaeric PDE5/6 catalytic domain, pH and temperature not specified in the publication Bos taurus