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Literature summary for 3.1.4.35 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)

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

Crystallization (Commentary)

Crystallization (Comment) Organism
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

Protein Variants Comment Organism
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

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

KM Value [mM]

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Purification (Commentary)

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

Substrates and Products (Substrate)

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

Synonyms

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

Turnover Number [1/s]

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

Ki Value [mM]

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