Phosphodiesterase (PDE) Assays and Profiling Services

CD Biosynsis offers comprehensive Phosphodiesterase (PDE) Assays essential for drug discovery programs targeting cyclic nucleotide signaling pathways. PDEs hydrolyze the second messengers cAMP and cGMP, making them crucial regulators of numerous cellular functions, including inflammation, cardiovascular health, and nervous system activity. Our platform provides high-quality, quantitative characterization of enzyme activity and inhibitor potency (IC50, Ki) across all major PDE families. We utilize robust, high-throughput technologies such as radiometric assays, fluorescence polarization, and coupled enzyme assays to ensure reliable and reproducible results critical for lead optimization and selectivity profiling. Choose from our extensive library of validated human PDE subtypes (PDE1-PDE11) to build a custom profiling panel tailored to your project needs.

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Precision Profiling Across All PDE Subtypes

Phosphodiesterases (PDEs) are a superfamily of 11 distinct families (PDE1–PDE11), each with multiple splice variants, exhibiting diverse substrate specificities (cAMP, cGMP, or dual) and tissue distributions. Targeting a specific PDE subtype is critical for achieving therapeutic efficacy while minimizing off-target side effects. Our services are optimized to handle the complexity of these targets, providing detailed kinetic data and selectivity profiles. We offer flexibility, from single-target kinetic analysis (Km, Vmax, Ki) to large-scale, multiplexed screening across entire PDE families. By enabling the selection of specific subtypes, we empower researchers to confidently assess inhibitor potency, selectivity, and mechanism of action for drug candidates.

Phosphodiesterase (PDE) Subtype Profiling Options

Major cAMP/cGMP Hydrolyzing PDEs Dual-Specificity and Specialized PDEs Assay and Kinetic Modules

Major cAMP/cGMP Hydrolyzing PDEs (Examples)

Choose Specific PDE Subtypes for Profiling

Check the box next to the PDE subtype you wish to include in your customized assay panel:

PDE4D (Target for CNS/Inflammation)

PDE5A (Target for Cardiovascular/Erectile Dysfunction)

PDE7A (Target for Immunology)

PDE8A/B (Testis/Thyroid)

PDE10A (Target for Schizophrenia)

PDE11A (Dual Specificity)

PDE2A (Dual Specificity, Inhibited by cGMP)

All other 50+ PDE Subtypes (Inquire)

Dual-Specificity and Specialized PDEs

Choose Additional Subtypes for Selectivity Testing

Select additional PDE targets to assess selectivity and minimize off-target effects:

PDE1A (Ca2+/Calmodulin-dependent)

PDE3A (cAMP-specific, cGMP-inhibited)

PDE6C (Photoreceptor Specific)

PDE9A (cGMP-specific)

PDE4A

PDE4B

PDE4C

Complete PDE Family Panel (PDE1-PDE11)

Available Assay and Kinetic Modules

Select Quantitative and Mechanistic Services

IC50 Determination (Dose-Response)

Quantitative measurement of inhibitor potency against each selected PDE subtype across a concentration range.

Full Kinetic Analysis (Km, Vmax, Ki)

Precise determination of kinetic parameters and the inhibition constant (Ki), including detailed mechanism (competitive, non-competitive).

Selectivity Profiling

Cross-family profiling against a custom panel of 20+ PDE subtypes to determine selectivity index.

Phosphodiesterase (PDE) Profiling Workflow

A rigorous process from subtype validation to inhibitor characterization.

Target Subtype Selection and Sourcing

Assay Platform Optimization

Inhibitor Screening and Potency Confirmation

Advanced Kinetics and Reporting

Panel Customization: Finalize the list of specific PDE subtypes based on client selection and therapeutic area.

Enzyme Quality Control: Verify purity (> 90 percent) and baseline activity of all recombinant PDE enzymes (in-house or client-supplied).

Technology Selection: Choose the optimal detection method (e.g., Radiometric, FP, or coupled assay) based on substrate (cAMP/cGMP) and enzyme subtype.

Assay Optimization: Titrate enzyme and substrate (cAMP or cGMP) concentrations to ensure robust, linear kinetics and high Z-factor (> 0.7).

IC50 Determination: Perform dose-response curves for all test compounds against the customized PDE panel.

Lead Confirmation: Validate IC50 values in triplicate using the optimized assay conditions.

  • Mechanistic Analysis: Perform full kinetic studies at varying substrate concentrations to determine the Ki and inhibition mode.
  • Selectivity Index: Calculate specificity ratios based on the IC50 values across the entire custom panel.
  • Reporting: Deliver raw data, analyzed plots, IC50/Ki values, and full technical protocols.

Expertise in Cyclic Nucleotide Signaling

Extensive PDE Subtype Library

           

Access to validated recombinant PDE enzymes covering all 11 families and key splice variants for comprehensive selectivity.

Diverse Assay Technologies

           

Utilization of high-sensitivity radiometric, fluorescence polarization, and coupled assays for optimal PDE activity measurement.

Detailed Mechanistic Data

           

Accurate determination of Ki, competitive or non-competitive mode, and allosteric effects for inhibitor mechanism.

Custom Selectivity Profiling

           

Ability to choose specific off-target PDE subtypes to minimize toxicity risks and improve therapeutic window.

Client Testimonials on PDE Assays

"The selectivity profiling across PDE1-PDE11 confirmed the exquisite specificity of our lead compound for PDE4D, which was critical for minimizing cardiovascular risks."

Dr. Samuel Liu, Medicinal Chemistry Director

"Their full kinetic Ki determination clearly showed a non-competitive mechanism, guiding our scaffold design toward a novel allosteric binding site."

Ms. Anya Sharma, Preclinical Development Lead

"The high-throughput radiometric assay they optimized for PDE5A quickly delivered robust IC50 data for our entire screening library with excellent Z-factors."

Mr. Julian Chen, Therapeutic Discovery Lead

FAQs about Phosphodiesterase (PDE) Assays

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What are the key substrates for PDEs?

The key substrates for phosphodiesterases are the cyclic nucleotides, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). Different PDE families show preference for cAMP, cGMP, or both.

Why is PDE selectivity profiling important?

Due to the high sequence homology between PDE subtypes and their broad distribution, inhibiting an off-target PDE (e.g., PDE5) can lead to unwanted side effects (e.g., hypotension). Selectivity profiling ensures the compound targets the desired subtype.

How do you distinguish between cAMP- and cGMP-specific PDEs?

We use specific, validated assay conditions and substrates. For example, PDE4 is profiled exclusively with cAMP, while PDE5 is profiled exclusively with cGMP. Dual-specificity enzymes (e.g., PDE1, 2, 3, 10, 11) are profiled against both substrates.

What is the advantage of a radiometric assay for PDE?

Radiometric assays (using 3H-cAMP/cGMP) offer extremely high sensitivity and low background noise, making them the gold standard for accurate kinetic analysis, especially for low-activity PDE subtypes.

How much does Metabolic Engineering services cost?

The cost of Metabolic Engineering services depends on the project scope, complexity of the target compound, the host organism chosen, and the required yield optimization. We provide customized quotes after a detailed discussion of your specific research objectives.

Do your engineered strains meet regulatory standards?

We adhere to high quality control standards in all strain construction and optimization processes. While we do not handle final regulatory approval, our detailed documentation and compliance with best laboratory practices ensure your engineered strains are prepared for necessary regulatory filings (e.g., GRAS, FDA).

What to look for when selecting the best gene editing service?

We provide various gene editing services such as CRISPR-sgRNA library generation, stable transformation cell line generation, gene knockout cell line generation, and gene point mutation cell line generation. Users are free to select the type of service that suits their research.

Does gene editing allow customisability?

Yes, we offer very customised gene editing solutions such as AAV vector capsid directed evolution, mRNA vector gene delivery, library creation, promoter evolution and screening, etc.

What is the process for keeping data private and confidential?

We adhere to the data privacy policy completely, and all customer data and experimental data are kept confidential.

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