PDE4D2 Assay Service
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Target
PDE4D2
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Description
Screening and/or profiling inhibitor compounds against PDE4D2 phosphodiesterase activity in a biochemical assay.
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Synonyms
PDE4D, PDE4-D2, phosphodiesterase 4D2
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Example Data
*Example only, final data may vary.
Assay Details
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Assay Format
Fluorescence Polarization
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Reference Compounds and IC50
Apremilast, 0.1 μM; Crisaborole, 0.8 μM; Rolipram, 0.2 μM
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Assay Principle
The PDE4D2 Assay is designed for identification of inhibitors of PDE4D2 using fluorescence polarization. The assay is based on the binding of a fluorescent nucleotide monophosphate generated by PDE4D2 to the binding agent. The key to the PDE4D2 Assay is the specific binding agent. In this assay, only two simple steps on a microtiter plate are required for PDE4D2 reactions. First, the fluorescently labeled cAMP is incubated with a sample containing PDE4D2 for 1 hour. Second, a binding agent is added to the reaction mix to produce a change in fluorescent polarization that can then be measured using a fluorescence reader equipped for the measurement of fluorescence polarization.
Target Details
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Protein Family
Phosphodiesterases
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UniProt
Q08499-5
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Background
Phosphodiesterases (PDEs) play an important role in the dynamic regulation of cAMP and cGMP signaling. PDE4D is a regulator of airway smooth-muscle contractility, and has been identified as a potential risk predictor for ischemic stroke. Additionally, PDE4D has been associated with asthma pathophysiology and bone formation. The PDE4D gene encodes at least 9 different isoforms. Phosphodiesterases catalyze the hydrolysis of the phosphodiester bond in dye-labeled cyclic monophosphates.
Delivery
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Estimated Turnaround
Two to three weeks following delivery of compounds
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Results
Extensive report with raw and analyzed data, graphs, and detailed protocols. Includes positive control for inhibition.
