Bromodomain Screening Service

Bromodomains are critical epigenetic "reader" modules that recognize acetylated lysine residues on histones and other proteins, playing a key role in regulating gene expression and cellular processes. Their involvement in diseases such as cancer, inflammation, and metabolic disorders makes them promising therapeutic targets. CD BioSciences offers specialized bromodomain screening services to help researchers and drug developers efficiently identify and validate inhibitors, accelerating the path from target validation to lead compound discovery.

Overview of Bromodomain

Bromodomains are conserved protein domains that function as epigenetic readers by specifically binding to acetylated lysine residues, primarily on histone tails. This interaction facilitates the recruitment of transcriptional co-regulators and chromatin-modifying complexes, thereby influencing gene expression, DNA repair, and cell cycle progression. Due to their central role in epigenetic regulation and their dysregulation in various diseases—particularly in cancers driven by BET family proteins (e.g., BRD4)—bromodomains have emerged as high-value therapeutic targets. Screening for selective bromodomain inhibitors is essential not only for drug discovery but also for understanding the mechanistic roles of these readers in biology and disease.

Fig.1 Structural features of the bromodomain binding pocket. (Boyson S P, et al., 2021)

Our Services

As a leading provider of epigenetic research services, CD BioSciences offers end-to-end bromodomain screening solutions tailored to meet the diverse needs of academic, biotech, and pharmaceutical researchers. Our platform integrates cutting-edge technology with deep expertise in assay development and data analysis, providing reliable, high-throughput solutions for inhibitor identification, selectivity profiling, and functional validation. Whether you are exploring novel chemical scaffolds or optimizing lead candidates, we deliver actionable data to accelerate your research and drug discovery initiatives.

Customized Solution for Bromodomain Screening

At CD BioSciences, we develop tailored screening solutions by integrating a suite of advanced technologies to meet your specific research goals. We utilize high-sensitivity biochemical assays such as AlphaScreen and TR-FRET for primary screening, complemented by biophysical validation methods including surface plasmon resonance (SPR) and microscale thermophoresis (MST). For functional insight, we employ cellular reporter assays and phenotypic screening. This multi-platform approach ensures robust hit identification and comprehensive characterization of bromodomain inhibitors.

Target Coverage

1. BET Family Bromodomains: BRD2, BRD3, BRD4 (BD1 and BD2), BRDT
2. Non-BET Bromodomains: CBP/p300, TAF1, ATAD2, BRD9, TRIM24, BAZ2B, MLL, ASH1L, BRPF1, and others
3. Custom & Challenging Targets: Client-provided bromodomain proteins, specific mutant variants and low-expression or unstable bromodomain proteins.

Available Screening Services

1. Primary High-Throughput Screening (HTS): Screening of diverse compound libraries (small molecules, fragments, natural products), concentration-response testing for hit confirmation.
2. Selectivity & Profiling Services: Counter-screening against related bromodomain families, pan-bromodomain selectivity profiling, kinase and GPCR panel screening to assess off-target effects.
3. Mechanistic & Advanced Characterization: Binding affinity (Kd) and kinetics (Kon/Koff) determination, competition assays with native acetyl-lysine peptides, cellular target engagement validation.
4. Integrated Hit-to-Lead Support: Structure-activity relationship (SAR) analysis, medicinal chemistry consultation, crystallography and computational modeling support.

Workflow of Bromodomain Screening Service

Consultation & Project Design

We begin with a comprehensive discussion to understand your specific bromodomain target, compound library characteristics, screening objectives (e.g., inhibitor discovery, selectivity profiling), and project scope. Based on this, we design a customized screening strategy, including assay selection, control setup, and key deliverables.

Assay Development & Optimization

Our scientists develop and rigorously optimize a robust biochemical or cellular assay tailored to your target. This includes validating recombinant bromodomain protein activity, optimizing buffer conditions, substrate concentrations, and signal-to-noise ratios, and establishing reproducibility through pilot screening runs.

Screening Execution & Quality Control

The validated assay is deployed for high-throughput or focused screening. Each batch includes standardized positive/negative controls, reference inhibitors, and replicate testing. We monitor key quality metrics such as Z'-factor throughout the process to ensure data integrity and reliability.

Hit Identification & Validation

Primary screening data are analyzed to identify initial hits based on statistical thresholds. These hits undergo dose-response confirmation testing to determine potency (IC₅₀). False positives are further excluded through counter-screening and orthogonal assay validation as needed.

Reporting & Follow-up Strategy

We provide a detailed technical report containing all experimental protocols, raw and analyzed data, dose-response curves, selectivity profiles, and a clear summary of validated hits. Our team is available for follow-up consultation to discuss hit prioritization, further characterization, or lead optimization strategies.

Our Advantages

1. Comprehensive Target Coverage: We support screening for both BET and non-BET bromodomain families, offering broad access to key epigenetic reader targets implicated in diverse diseases.
2. Integrated and Customizable Platform: Our end-to-end workflow—from assay development to advanced characterization—can be fully tailored to your specific research goals, library types, and throughput requirements.
3. High-Quality and Reproducible Data: We ensure reliability through validated reagents, optimized assay conditions, stringent quality controls, and orthogonal validation steps at key stages of the screening process.
4. Expert Support and Fast Turnaround: Our experienced scientific team provides dedicated project guidance and timely communication, delivering actionable results within agreed timelines to accelerate your discovery pipeline.

While bromodomains represent a key class of epigenetic readers, CD BioSciences also provides comprehensive screening services for other critical reader domains—including chromodomain, MBT domain, PHD finger, SRA domain, and Tudor domain, as well as integrated multiple domains screening—delivering a fully customizable and holistic platform for all your epigenetic target discovery needs. Contact us today to learn how our expertise can accelerate your research and drug development programs.

Reference

1. Boyson S P, Gao C, Quinn K, et al. Functional roles of bromodomain proteins in cancer[J]. Cancers, 2021, 13(14): 3606.