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Phosphodiesterase 4D - PDE4D2

Target Class Non-Kinase Enzymes FamilyPhosphodiesterase
SpeciesHuman   
Background
This gene encodes one of four mammalian counterparts to the fruit fly 'dunce' gene. The encoded protein has 3',5'-cyclic-AMP phosphodiesterase activity and degrades cAMP, which acts as a signal transduction molecule in multiple cell types. This gene uses different promoters to generate multiple alternatively spliced transcript variants that encode functional proteins.[provided by RefSeq, Sep 2009]

Protein Source
Human(recombinant): Expressed in Sf9 insect cells using baculovirus
Readout
Enzymatic Activity
Method
Detect conversion of cAMP to AMP using DiscoverX cAMP luminescent readout
Substrate
cAMP
Agonist Effect (Activation)
insufficient information
Antagonist Effect (Inhibition)
anti-inflammatory activities; antidepressant-like activities; emesis; vasculitis and arteritis; possible thymus atrophy
Ref.
Bowes et. al. 2012
AntagonistIC50(nM)
Rolipram160
Ro 20-17243500
Cilomilast40
Roflumilast0.3
Enzyme and test compound are preincubated for 15 minutes at room temp before substrate addition. cAMP substrate (at a concentration equal to EC80) is added and incubated at room temperature for 30 minutes. Enzyme reaction is terminated by addition of 9 mM IBMX. Signal is detected using the HitHunter® cAMP detection kit.
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For additional GPCR targets, please click here.

For additional kinase targets, please click here.