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Literature summary for 3.1.4.53 extracted from

  • Wang, H.; Peng, M.S.; Chen, Y.; Geng, J.; Robinson, H.; Houslay, M.D.; Cai, J.; Ke, H.
    Structures of the four subfamilies of phosphodiesterase-4 provide insight into the selectivity of their inhibitors (2007), Biochem. J., 408, 193-201.
    View publication on PubMedView publication on EuropePMC
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Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitor 4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid, comparison with isoforms PDE4A, PDE4B, PDE4C. Inhibitor binds in the same conformation to the deep cAMP substrate pocket and interacts with the same residues in each instance. Detailed structural comparison Homo sapiens
in complex with inhibitor 4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid, comparison with isoforms PDE4A, PDE4C, PDE4D. Inhibitor binds in the same conformation to the deep cAMP substrate pocket and interacts with the same resiudues in each instance. Detailed structural comparison Homo sapiens
in complex with inhibitor 4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid, comparison with isoforms PDE4B, PDE4C, PDE4D. Inhibitor binds in the same conformation to the deep cAMP substrate pocket and interacts with the same residues in each instance. Detailed structural comparison Homo sapiens
unliganded, detailed structural comparison with isoforms PDE4A, PDE4B, PDE4C Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid i.e. NVP; i.e. NVP; i.e. NVP Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0008
-
 cAMP pH 7.5, 25°C Homo sapiens
0.0015
-
 cAMP pH 7.5, 25°C Homo sapiens
0.0045
-
 cAMP pH 7.5, 25°C Homo sapiens
0.0051
-
 cAMP pH 7.5, 25°C Homo sapiens
0.24
-
 cGMP pH 7.5, 25°C Homo sapiens
0.427
-
 cGMP pH 7.5, 25°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 isoform PDE4B2B
-
Homo sapiens
-
 isoform PDE4C2
-
Homo sapiens P27815 isoform PDE4A10
-
Homo sapiens Q08499 isoform PDE4D2
-

Substrates and Products (Substrate)

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

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.48
-
 cGMP pH 7.5, 25°C Homo sapiens
0.66
-
 cAMP pH 7.5, 25°C Homo sapiens
1.19
-
 cGMP pH 7.5, 25°C Homo sapiens
1.56
-
 cAMP pH 7.5, 25°C Homo sapiens
5.4
-
 cAMP pH 7.5, 25°C Homo sapiens
6.7
-
 cAMP pH 7.5, 25°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00057
-
 pH 7.5, 25°C Homo sapiens 4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid
0.00065
-
 pH 7.5, 25°C Homo sapiens 4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid
0.0033
-
 pH 7.5, 25°C Homo sapiens 4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid
0.0057
-
 pH 7.5, 25°C Homo sapiens 4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid