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Literature summary for 3.1.4.53 extracted from

  • Schafer, P.H.; Parton, A.; Gandhi, A.K.; Capone, L.; Adams, M.; Wu, L.; Bartlett, J.B.; Loveland, M.A.; Gilhar, A.; Cheung, Y.F.; Baillie, G.S.; Houslay, M.D.; Man, H.W.; Muller, G.W.; Stirling, D.I.
    Apremilast, a cAMP phosphodiesterase-4 inhibitor, demonstrates anti-inflammatory activity in vitro and in a model of psoriasis (2010), Br. J. Pharmacol., 159, 842-855.
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
apremilast CC-10004, i.e. (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]acetamide, oral phosphodiesterase-4 inhibitor, apremilast shows no marked selectivity among PDE4 isozymes Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3',5'-cAMP + H2O Homo sapiens
-
 5'-AMP
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
gel filtration Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
peripheral blood mononuclear cell
-
 Homo sapiens
-
U-937 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
cAMP phosphodiesterase-4
-
 Homo sapiens
PDE4
-
 Homo sapiens
PDE4A4 isoform Homo sapiens
PDE4B2 isoform Homo sapiens
PDE4C2 isoform Homo sapiens
PDE4D3 isoform Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000068
-
 apremilast PDE4 purified from U-937 cells, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00002
-
 recombinant isoform PDE4A4, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication Homo sapiens apremilast
0.00003
-
 recombinant isoform PDE4D3, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication Homo sapiens apremilast
0.000049
-
 recombinant isoform PDE4B2, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication Homo sapiens apremilast
0.00005
-
 recombinant isoform PDE4C2, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication Homo sapiens apremilast
0.000074
-
 PDE4 purified from U-937 cells, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication Homo sapiens apremilast