Poly(ADP-ribose) Polymerase (PARP) Assays and Profiling

CD Biosynsis offers comprehensive Poly(ADP-ribose) Polymerase (PARP) Assays and Profiling Services, essential for drug discovery targeting DNA repair pathways, particularly in oncology. The PARP enzyme family is critical for detecting and signaling DNA damage, making specific PARP inhibitors a cornerstone of modern cancer therapy (e.g., synthetic lethality strategies). Our platform provides quantitative analysis of PARP catalytic activity, inhibitor potency (IC50, Ki), and selectivity across the entire PARP family. We utilize highly sensitive detection methods, including colorimetric, fluorescence-based, and AlphaLISA assays, ensuring high throughput and robust data quality. We provide researchers with the ability to selectively profile compounds against specific PARP targets, accelerating the development of potent and selective PARP inhibitors.

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Targeting the DNA Damage Response Pathway

PARP enzymes catalyze the transfer of ADP-ribose moieties from NAD+ onto acceptor proteins, a process known as PARylation. This modification is crucial for DNA repair (PARP1, PARP2) but also plays roles in gene regulation, inflammation, and cell death (other PARP members). Accurate profiling is necessary to ensure inhibitors are selective for the therapeutic targets (like PARP1) while minimizing off-target effects on non-therapeutic PARP enzymes. Our platform offers access to purified, validated recombinant proteins for nearly all PARP family members, enabling researchers to build custom assay panels tailored to their specific drug discovery goals. This flexible approach supports both initial high-throughput screening and detailed mechanistic studies (e.g., competitive binding, allosteric modulation).

PARP Profiling Service Workflow

A structured process for rapid and reliable inhibitor characterization.

Enzyme and Panel Selection

Assay Optimization and Validation

Inhibitor Profiling (IC50)

Mechanistic Analysis and Reporting

Consultation: Determine the therapeutic target (e.g., PARP1) and the required selectivity panel based on client needs.

Enzyme Sourcing: Acquire or prepare highly pure, validated recombinant enzymes for all selected PARP members.

Assay Setup: Establish optimal concentrations of enzyme, NAD+, and DNA substrate (if required) for each target PARP.

Validation: Confirm assay robustness using established controls and high Z-factor analysis (> 0.7).

Compound Screening: Run 8- or 10-point dose-response curves for test compounds against the selected panel members.

Data Fitting: Calculate the half maximal inhibitory concentration (IC50) for all test compounds against all targets.

Ki Determination: Conduct full kinetic studies on top hits to determine the inhibition constant (Ki).
Selectivity Index: Calculate the selectivity ratio (e.g., IC50 of PARP5a / IC50 of PARP1).
Reporting: Deliver raw data, analyzed IC50/Ki plots, and a detailed technical report.

Precision and Selectivity in PARP Inhibitor Development

Complete PARP Family Panel

Access to nearly all 17 human PARP family members for comprehensive off-target selectivity screening.

Customizable Assays

Ability to freely select and combine target PARP enzymes to build a bespoke profiling panel for focused research.

Mechanistic Insight (Ki)

Precise kinetic analysis to define the mechanism of inhibition (e.g., NAD+ competitive or allosteric).

High-Throughput Capability

Automated screening platforms for rapid and robust IC50 determination of large compound libraries.

Client Testimonials on PARP Assays

"The customizable PARP panel was exactly what we needed. We quickly ruled out Tankyrase activity in our PARP1 lead, confirming high selectivity early in the pipeline."

Dr. Jian Li, Medicinal Chemistry

"The Ki determination provided crucial proof that our compound was a true NAD+ competitive inhibitor, which guided our compound optimization efforts successfully."

Ms. Nicole Smith, Oncology R&D Manager

"Their high-throughput PARP assay was robust, achieving a high Z-factor across all 10 PARP family members we selected, allowing us to screen our library efficiently."

Mr. Alex Davies, Therapeutic Discovery Lead

FAQs about PARP Assays

Still have questions?

What is the difference between PARP1 and Tankyrase (PARP5a/b) inhibitors?

PARP1 is primarily involved in DNA damage repair, while Tankyrases (PARP5a/b) are involved in Wnt signaling pathway regulation. Selectivity is critical; therapeutic inhibitors often target PARP1, while Tankyrase inhibitors are being explored for different applications.

What is the substrate for PARP enzymes in the assay?

The primary substrate is NAD+ (Nicotinamide adenine dinucleotide), which provides the ADP-ribose moiety for PARylation. Assays monitor the consumption of NAD+ or the incorporation of ADP-ribose.

Why do PARP1 and PARP2 assays require DNA activation?

PARP1 and PARP2 are intrinsically active only when they bind to damaged DNA (e.g., DNA nicks or breaks). Assays for these targets require the addition of activated DNA (often pre-nicked DNA) to achieve full activity and physiological relevance.

Can you distinguish between NAD+ competitive and allosteric inhibitors?

Yes. By conducting detailed kinetic studies at varying concentrations of both the inhibitor and the NAD+ substrate, we can determine the inhibition constant (Ki) and use Lineweaver-Burk or non-linear fitting to distinguish between competitive and allosteric modes.

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.

Poly(ADP-ribose) Polymerase (PARP) Assays and Profiling

Targeting the DNA Damage Response Pathway

PARP Family Selectivity Profiling Options

Essential Targets for DNA Damage Repair (DDR)

Selectable Core Assays

Other Key Regulatory PARP Targets

Selectable Secondary Assays

Assay Options for All Selected Targets

Available Profiling Services

PARP Profiling Service Workflow

Precision and Selectivity in PARP Inhibitor Development

Client Testimonials on PARP Assays

FAQs about PARP Assays