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Literature summary 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

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.4.53 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)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.1.4.53 3',5'-cAMP + H2O Homo sapiens
-
 5'-AMP
-
 ?

Organism

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

Purification (Commentary)

EC Number Purification (Comment) Organism
3.1.4.53 gel filtration Homo sapiens

Source Tissue

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.4.53 3',5'-cAMP + H2O
-
 Homo sapiens 5'-AMP
-
 ?

Synonyms

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

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.1.4.53 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

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.4.53 0.00002
-
 recombinant isoform PDE4A4, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication Homo sapiens apremilast
3.1.4.53 0.00003
-
 recombinant isoform PDE4D3, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication Homo sapiens apremilast
3.1.4.53 0.000049
-
 recombinant isoform PDE4B2, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication Homo sapiens apremilast
3.1.4.53 0.00005
-
 recombinant isoform PDE4C2, using 0.001 mM cAMP as substrate, pH and temperature not specified in the publication Homo sapiens apremilast
3.1.4.53 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