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Literature summary for 3.1.4.17 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
Search for more literature for 3.1.4.17

Cloned(Commentary)

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

Protein Variants

Protein Variants Comment Organism
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

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
nickel resin column chromatography Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
blood platelet
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3',5'-cAMP + H2O 3',5'-cAMP is predominantly hydrolyzed by PDE3A Homo sapiens 5'-AMP
-
 ?
3',5'-cGMP + H2O
-
 Homo sapiens 5'-GMP
-
 ?
additional information NAD+ is not a substrate of PDE3A Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
cAMP phosphodiesterase
-
 Homo sapiens
PDE3A
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
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