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Literature summary for 3.1.4.35 extracted from

  • Zoraghi, R.; Francis, S.H.; Corbin, J.D.
    Critical amino acids in phosphodiesterase-5 catalytic site that provide for high-affinity interaction with cyclic guanosine monophosphate and inhibitors (2007), Biochemistry, 46, 13554-13563.
    View publication on PubMed
Search for more literature for 3.1.4.35

Cloned(Commentary)

Cloned (Comment) Organism
expression of his-tagged protein in baculovirus/Sf9 system Homo sapiens

Protein Variants

Protein Variants Comment Organism
F786A modest decrease in affinities for substrate cGMP and inhibitors vardenafil, sildenafil, tadalafil, 3-isobutyl-1-methylxanthine Homo sapiens
F820A decrease in affinities for substrate cGMP and inhibitors vardenafil, sildenafil, tadalafil, 3-isobutyl-1-methylxanthine Homo sapiens
H613A modest decrease in affinities for substrate cGMP and inhibitors vardenafil, sildenafil, tadalafil, 3-isobutyl-1-methylxanthine Homo sapiens
L765A modest decrease in affinities for substrate cGMP and inhibitors vardenafil, sildenafil, tadalafil, 3-isobutyl-1-methylxanthine Homo sapiens
Q817A decrease in affinities for substrate cGMP and inhibitors vardenafil, sildenafil, tadalafil, 3-isobutyl-1-methylxanthine Homo sapiens
V782A decrease in affinities for substrate cGMP and inhibitors vardenafil, sildenafil, tadalafil, 3-isobutyl-1-methylxanthine Homo sapiens
Y612A decrease in affinities for substrate cGMP and inhibitors vardenafil, sildenafil, tadalafil, 3-isobutyl-1-methylxanthine Homo sapiens
Y612F modest decrease in affinities for substrate cGMP and inhibitors vardenafil, sildenafil, tadalafil, 3-isobutyl-1-methylxanthine Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-isobutyl-1-methylxanthine
-
 Homo sapiens
sildenafil
-
 Homo sapiens
tadalafil
-
 Homo sapiens
vardenafil
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0029
-
 cGMP wild-type, pH 7.5, 30°C Homo sapiens
0.0061
-
 cGMP mutant Y612F, pH 7.5, 30°C Homo sapiens
0.0071
-
 cGMP mutant H613A, pH 7.5, 30°C Homo sapiens
0.0159
-
 cGMP mutant V782A, pH 7.5, 30°C Homo sapiens
0.0277
-
 cGMP mutant L765A, pH 7.5, 30°C Homo sapiens
0.0297
-
 cGMP mutant F786A, pH 7.5, 30°C Homo sapiens
0.0416
-
 cGMP mutant Y612A, pH 7.5, 30°C Homo sapiens
0.172
-
 cGMP mutant F820A, pH 7.5, 30°C Homo sapiens
0.182
-
 cGMP mutant Q817A, pH 7.5, 30°C Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
99000
-
 x * 99000, SDS-PAGE of recombinant His-tagged protein Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens O76074 isoform PDE5A1
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
cGMP + H2O
-
 Homo sapiens 5'-GMP
-
 ?

Subunits

Subunits Comment Organism
? x * 99000, SDS-PAGE of recombinant His-tagged protein Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.00083
-
 cGMP mutant H613A, pH 7.5, 30°C Homo sapiens
0.04
-
 cGMP mutant F820A, pH 7.5, 30°C Homo sapiens
0.8
-
 cGMP mutant Y612A, pH 7.5, 30°C Homo sapiens
1.3
-
 cGMP mutant L765A, pH 7.5, 30°C Homo sapiens
1.7
-
 cGMP mutant Y612F, pH 7.5, 30°C Homo sapiens
2.2
-
 cGMP wild-type, pH 7.5, 30°C Homo sapiens
2.5
-
 cGMP mutant V782A, pH 7.5, 30°C Homo sapiens
3.7
-
 cGMP mutant F786A, pH 7.5, 30°C Homo sapiens
3.8
-
 cGMP mutant Q817A, pH 7.5, 30°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000006
-
 mutant Y612F, pH 7.5, 30°C Homo sapiens vardenafil
0.00000012
-
 wild-type, pH 7.5, 30°C Homo sapiens vardenafil
0.00000049
-
 mutant L765A, pH 7.5, 30°C Homo sapiens vardenafil
0.00000078
-
 mutant H613A, pH 7.5, 30°C Homo sapiens vardenafil
0.00000083
-
 mutant F786A, pH 7.5, 30°C Homo sapiens vardenafil
0.0000013
-
 mutant Y612F, pH 7.5, 30°C Homo sapiens sildenafil
0.0000019
-
 mutant Y612F, pH 7.5, 30°C Homo sapiens 3-isobutyl-1-methylxanthine
0.0000022
-
 wild-type, pH 7.5, 30°C Homo sapiens tadalafil
0.000003
-
 mutant L765A, pH 7.5, 30°C Homo sapiens 3-isobutyl-1-methylxanthine
0.0000033
-
 wild-type, pH 7.5, 30°C Homo sapiens sildenafil
0.0000035
-
 wild-type, pH 7.5, 30°C Homo sapiens 3-isobutyl-1-methylxanthine
0.0000058
-
 mutant Y612F, pH 7.5, 30°C Homo sapiens tadalafil
0.0000067
-
 mutant V782A, pH 7.5, 30°C Homo sapiens tadalafil
0.0000091
-
 mutant L765A, pH 7.5, 30°C Homo sapiens tadalafil
0.0000101
-
 mutant L765A, pH 7.5, 30°C Homo sapiens sildenafil
0.0000132
-
 mutant H613A, pH 7.5, 30°C Homo sapiens sildenafil
0.0000147
-
 mutant Y612A, pH 7.5, 30°C Homo sapiens vardenafil
0.0000206
-
 mutant F786A, pH 7.5, 30°C Homo sapiens sildenafil
0.0000275
-
 mutant V782A, pH 7.5, 30°C Homo sapiens vardenafil
0.0000319
-
 mutant V782A, pH 7.5, 30°C Homo sapiens sildenafil
0.0000375
-
 mutant F786A, pH 7.5, 30°C Homo sapiens tadalafil
0.0000423
-
 mutant H613A, pH 7.5, 30°C Homo sapiens 3-isobutyl-1-methylxanthine
0.0000425
-
 mutant V782A, pH 7.5, 30°C Homo sapiens 3-isobutyl-1-methylxanthine
0.0000433
-
 mutant F786A, pH 7.5, 30°C Homo sapiens 3-isobutyl-1-methylxanthine
0.0000537
-
 mutant F820A, pH 7.5, 30°C Homo sapiens vardenafil
0.0000613
-
 mutant Q817A, pH 7.5, 30°C Homo sapiens vardenafil
0.000081
-
 mutant H613A, pH 7.5, 30°C Homo sapiens tadalafil
0.0000983
-
 mutant Y612A, pH 7.5, 30°C Homo sapiens sildenafil
0.000112
-
 mutant Y612A, pH 7.5, 30°C Homo sapiens tadalafil
0.000141
-
 mutant Q817A, pH 7.5, 30°C Homo sapiens sildenafil
0.000152
-
 mutant Y612A, pH 7.5, 30°C Homo sapiens 3-isobutyl-1-methylxanthine
0.00021
-
 mutant Q817A, pH 7.5, 30°C Homo sapiens tadalafil
0.000214
-
 mutant Q817A, pH 7.5, 30°C Homo sapiens 3-isobutyl-1-methylxanthine
0.000235
-
 mutant F820A, pH 7.5, 30°C Homo sapiens sildenafil
0.000301
-
 mutant F820A, pH 7.5, 30°C Homo sapiens tadalafil
0.000327
-
 mutant F820A, pH 7.5, 30°C Homo sapiens 3-isobutyl-1-methylxanthine