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Literature summary extracted from

  • Dunkern, T.R.; Hatzelmann, A.
    Characterization of inhibitors of phosphodiesterase 1C on a human cellular system (2007), FEBS J., 274, 4812-4824.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.4.17 (6aS,9aR)-3-benzyl-2-(biphenyl-4-ylmethyl)-5-methyl-5,6a,7,8,9,9a-hexahydrocyclopenta[4,5]imidazo[2,1-b]purin-4(3H)-one comparison of inhibitory effect on several recombinant human PDE isoforms. Effective PDE1 inhibitor in cellular context Homo sapiens
3.1.4.17 3'-benzyl-2'-(biphenyl-4-ylmethyl)-5'-methyl-3'H-spiro[cyclopentane-1,7'-imidazo[2,1-b]purin]-4'(5'H)-one comparison of inhibitory effect on several recombinant human PDE isoforms. Effective PDE1 inhibitor in cellular context Homo sapiens
3.1.4.17 3-isobutyl-8-(methoxymethyl)-1-methyl-3,9-dihydro-1H-purine-2,6-dione i.e. 8MM-IBMX, comparison of inhibitory effect on several recombinant human PDE isoforms Homo sapiens
3.1.4.17 5-methyl-2-[4-(trifluoromethyl)benzyl]-5,6a,7,8,9,9a-hexahydrocyclopenta[4,5]imidazo[2,1-b]purin-4(1H)-one i.e. SCH51866, comparison of inhibitory effect on several recombinant human PDE isoforms. Effective PDE1 inhibitor in cellular context Homo sapiens
3.1.4.17 vinpocetine comparison of inhibitory effect on several recombinant human PDE isoforms Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.1.4.17 0.0013
-
 cGMP isoform PDE1C, pH 7.4 Homo sapiens
3.1.4.17 0.0017
-
 cAMP isoform PDE1C, pH 7.4 Homo sapiens

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
3.1.4.17 72000
-
 x * 72000, splice variant PDE1C1, x * 75000, splice variant PDE1C3 Homo sapiens
3.1.4.17 75000
-
 x * 72000, splice variant PDE1C1, x * 75000, splice variant PDE1C3 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.1.4.17 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.4.17 A-172 cell glioblastoma cell, expression of isoform PDE1C and lower levels of isoforms PDE2, PDE3, PDE4, and PDE5 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.4.17 3',5'-cAMP + H2O
-
 Homo sapiens 5'-AMP
-
 ?
3.1.4.17 3',5'-cGMP + H2O
-
 Homo sapiens 5'-GMP
-
 ?

Subunits

EC Number Subunits Comment Organism
3.1.4.17 ? x * 72000, splice variant PDE1C1, x * 75000, splice variant PDE1C3 Homo sapiens