Phosphodiesterase 3A - PDE3A

Target Class Non-Kinase Enzymes FamilyPhosphodiesterase
SpeciesHuman   
Background
This gene encodes a member of the cGMP-inhibited cyclic nucleotide phosphodiesterase (cGI-PDE) family. cGI-PDE enzymes hydrolyze both cAMP and cGMP, and play critical roles in many cellular processes by regulating the amplitude and duration of intracellular cyclic nucleotide signals. The encoded protein mediates platelet aggregation and also plays important roles in cardiovascular function by regulating vascular smooth muscle contraction and relaxation. Inhibitors of the encoded protein may be effective in treating congestive heart failure. Alternatively spliced transcript variants encoding multiple isoforms have been observed for this gene. [provided by RefSeq, Sep 2011]

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)
increase cardiac contractility; increase HR; decrease BP; thrombocytopaenia; ventricular arrhythmia
Ref.
Bowes et. al. 2012
AntagonistIC50(nM)
Cilostamide33
IBMX1400
Milrinone 260
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.
For other SAFETYscan assays, please click here.

For additional GPCR targets, please click here.

For additional kinase targets, please click here.