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Literature summary extracted from

  • Hung, S.H.; Liu, A.H.; Pixley, R.A.; Francis, P.; Williams, L.D.; Matsko, C.M.; Barnes, K.D.; Sivendran, S.; Colman, R.F.; Colman, R.W.
    A new nonhydrolyzable reactive cGMP analogue, (Rp)-guanosine-3,5-cyclic-S-(4-bromo-2,3-dioxobutyl)monophosphorothioate, which targets the cGMP binding site of human platelet PDE3A (2008), Bioorg. Chem., 36, 141-147.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.1.4.17 expressed in a baculovirus/insect cell Sf9 system Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
3.1.4.17 additional information amino acid residues N845, E866, E971, F972, and F1004 are involved in cAMP (substrate) binding, while Y751, H836, H840, E866, D950 and F1004 participate in cGMP (inhibitor) binding Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.4.17 (Rp)-guanosine-3',5'-cyclic-S-(4-bromo-2,3-dioxobutyl)monophosphorothioate time-dependent and irreversible inactivation of PDE3A Homo sapiens
3.1.4.17 cGMP competitive inhibitor of PDE3A acting directly at the catalytic site Homo sapiens
3.1.4.17 additional information NAD+ is not an inhibitor of PDE3A Homo sapiens

Organism

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

Purification (Commentary)

EC Number Purification (Comment) Organism
3.1.4.17 nickel resin column chromatography Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.4.17 blood platelet
-
 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 3',5'-cAMP is predominantly hydrolyzed by PDE3A Homo sapiens 5'-AMP
-
 ?
3.1.4.17 3',5'-cGMP + H2O
-
 Homo sapiens 5'-GMP
-
 ?
3.1.4.17 additional information NAD+ is not a substrate of PDE3A Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.4.17 cAMP phosphodiesterase
-
 Homo sapiens
3.1.4.17 PDE3A
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.1.4.17 0.0434
-
 (Rp)-guanosine-3',5'-cyclic-S-(4-bromo-2,3-dioxobutyl)monophosphorothioate in 45 mM HEPES (pH 7.2), 20 mM MgCl2, and 4 mM MES, at 25°C Homo sapiens