Enzyme Activity Screening Service

Navigating the complexities of epigenetic target validation and inhibitor discovery requires specialized tools and deep expertise. The comprehensive epigenetic enzyme activity screening service provided by CD BioSciences is designed to meet this need, delivering reliable, high-quality data to accelerate your research and drive your drug discovery pipeline forward. With our customized, robust platform, you can efficiently identify and characterize novel modulators of key epigenetic enzymes.

Key Epigenetic Enzyme Target Families

In epigenetic regulation, enzymes serve as the master "writers" and "erasers" that dynamically install or remove chemical modifications—such as methylation, acetylation, ADP-ribosylation, and ubiquitination—on DNA, RNA, and histone proteins. By precisely controlling these reversible marks, enzymes directly influence chromatin structure, gene expression, and cellular identity without altering the underlying genetic code. Given their central role in development, differentiation, and disease pathogenesis—especially in cancer, neurological disorders, and immune dysregulation—these enzymes represent highly promising therapeutic targets. Screening for modulators of their activity is therefore a critical first step in drug discovery, chemical probe development, and mechanistic research. The table below summarizes the core enzyme target families that are currently receiving significant attention in epigenetic drug development and functional research.

* Note: Many of these enzymes also target non-histone proteins, expanding their regulatory scope beyond traditional epigenetics.

Significance of Epigenetic Enzyme Activity Screening

Epigenetic enzyme activity screening holds paramount significance as the cornerstone for discovering novel therapeutics and deciphering fundamental biological mechanisms. By enabling the high-throughput identification and characterization of small-molecule modulators—inhibitors or activators—for key "writer" and "eraser" enzymes, this screening directly fuels target validation, lead compound optimization, and the development of chemical probes. This process is indispensable for translating our understanding of epigenetic dysregulation in diseases like cancer, neurological disorders, and inflammatory conditions into precision medicine strategies, ultimately accelerating the pipeline from basic research to clinical application.

Fig.1 Epigenetic mechanisms and key examples of widely studied modifications and their modifying enzymes. (Dai W, et al., 2024)

Our Services

Epigenetic enzyme activity screening often presents significant challenges, including the need for highly specialized assay development, access to purified active enzymes, optimization of complex reaction conditions, and reliable data interpretation. At CD BioSciences, we overcome these hurdles by providing a comprehensive, fully integrated epigenetic enzyme activity screening service. Our tailored platform delivers robust, high-quality data to accelerate your target validation, lead discovery, and mechanistic research.

One-stop Solution for Epigenetic Enzyme Activity Screening

CD BioSciences provides a comprehensive, end-to-end solution designed to streamline your drug discovery and biochemical research. From initial project consultation and customized assay design to high-quality experimental execution and in-depth data analysis with a final report, our service eliminates the technical hurdles and resource demands of in-house screening. We support activity screening and profiling for a broad spectrum of critical epigenetic enzyme families, accelerating your path to validated hits and novel insights. Our platform is validated for screening key epigenetic enzyme classes, including but not limited to:

Technical Methods and Testing Platforms

At CD BioSciences, we tailor our screening strategy to your specific target, project goals, and screening stage. Our scientific team recommends and implements the most suitable, robust detection method for each unique project, leveraging a diverse suite of industry-standard and advanced testing platforms to ensure high-quality, reliable data. Our technical arsenal includes leading methodologies such as:

1. Colorimetric/Fluorometric Assays: For direct, homogeneous detection of reaction products (e.g., NADH, released fluorophores). Ideal for high-throughput primary screening.
2. Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET): A gold-standard, homogeneous method offering exceptional sensitivity and low background for measuring enzymatic activity and binding interactions.
3. AlphaScreen/LISA Technology: A bead-based, no-wash platform perfect for studying protein-protein interactions, modifications, and weak binding events with high signal-to-noise ratios.
4. Radiometric Assays: Utilizing labeled substrates (³H, ¹⁴C) to deliver the highest sensitivity and direct measurement of enzymatic transfer, often used for validation and specialized applications.
5. Mass Spectrometry (MS)-Based Detection: For definitive, quantitative analysis of specific modification sites and stoichiometry, providing unparalleled mechanistic insight and confirmation.

Workflow of Epigenetic Enzyme Activity Screening Service

Service Application Scenarios

1. Drug Discovery and High-Throughput Screening (HTS): Screening large compound libraries to identify and profile potent, selective lead candidates against your epigenetic targets.
2. Chemical Probe and Tool Compound Development: Validating the specificity and mechanism of novel chemical probes to ensure reliable research tools.
3. Mechanistic and Functional Studies: Elucidating enzyme kinetics, inhibition mechanisms, and functional consequences of mutations or modifications.
4. Biomarker Discovery and Validation Support: Profiling epigenetic enzyme activity to identify and validate disease-relevant biomarkers across different biological contexts.
5. Identification of Active Ingredients in Natural Products: Isolating and validating bioactive natural compounds with specific epigenetic enzyme-modulating activity.

Our Advantages

1. Fully Customizable Workflow: Our assays can be tailored to accommodate various enzyme sources (e.g., recombinant proteins, cell lysates), substrates, and compound libraries (small molecules, natural products, fragment libraries).
2. Comprehensive Platform Coverage: We support screening across all key epigenetic enzyme families, including demethylases, methyltransferases, HATs/HDACs/SIRTs, PARPs, and DUBs.
3. High-Quality & Reliable Data: We ensure assay robustness by using validated active enzymes, optimized reaction conditions, and rigorous internal and external controls throughout the screening process.
4. Flexible Throughput Options: We offer both high-throughput screening for large-scale discovery and low-throughput formats for focused validation and detailed mechanistic studies.

With advanced technology and a professional team, CD BioSciences is committed to providing comprehensive epigenetic enzyme activity screening services to support your research and drug discovery journey. We combine extensive experience in assay development, advanced assay technologies, and a customer-centric workflow to ensure that every project delivers practical, high-quality results, from target validation to lead compound optimization. Contact us today to discuss how to customize our services to advance your specific research goals.

Reference

1. Dai W, Qiao X, Fang Y, et al. Epigenetics-targeted drugs: current paradigms and future challenges[J]. Signal Transduction and Targeted Therapy, 2024, 9(1): 332.