Chromodomains are critical epigenetic reader modules that specifically recognize methylated lysine residues on histone tails, playing essential roles in chromatin compaction, gene silencing, and cellular differentiation. Their dysregulation is closely linked to cancer progression and neurological disorders. CD BioSciences provides specialized chromodomain screening services to support targeted inhibitor discovery and functional studies of these key regulatory domains.
Chromodomains are evolutionarily conserved protein structural domains that function as methyl-lysine readers, primarily binding to methylated histone marks such as H3K9me3 and H3K27me3. These interactions facilitate the recruitment of chromatin-modifying complexes and are fundamental to processes like heterochromatin formation, transcriptional repression, and X-chromosome inactivation. Due to their central role in epigenetic regulation and their implication in diseases—particularly through Polycomb group proteins (e.g., CBX family) and heterochromatin protein 1 (HP1)—chromodomains have emerged as promising therapeutic targets. Screening for selective chromodomain inhibitors is crucial not only for developing novel epigenetic therapies but also for dissecting the biological functions of these readers in health and disease.
Fig.1 The chromatin domain protein CDYL acts as a crotonyl-CoA hydratase, regulating histone crotonylation and spermatogenesis. (Liu S, et al., 2017)
With expertise in epigenetic reader biology, CD BioSciences delivers end-to-end chromodomain screening solutions tailored to the needs of researchers in academia and industry. Our platform combines robust assay development, versatile screening technologies, and in-depth data analysis to identify and validate inhibitors targeting methyl-lysine recognition. Whether you aim to discover novel chemical probes or optimize lead compounds, we provide reliable, actionable data to advance your projects efficiently.
At CD BioSciences, we employ a multi-technology screening platform tailored for methyl-lysine reader targets, integrating high-throughput biochemical assays such as fluorescence polarization (FP) and AlphaScreen for primary compound screening, supported by surface plasmon resonance (SPR) and microscale thermophoresis (MST) for biophysical validation of binding affinity and kinetics. This robust approach ensures accurate identification and characterization of chromodomain-targeting inhibitors, accelerating your path from screening to validated leads.
Target Coverage
Analytical Services
This initial phase involves a detailed discussion to define your specific chromodomain target, research objectives (e.g., hit discovery or probe validation), compound library specifications, and key success metrics. Based on this, we co-develop a tailored project plan, including assay selection, throughput requirements, and deliverable timelines.
Our scientists establish and rigorously optimize a robust biochemical binding assay tailored to your target, such as a fluorescence polarization (FP) competition assay. This step includes validating the activity of recombinant chromodomain proteins, titrating methylated peptide probes, optimizing buffer conditions for signal stability, and confirming assay reproducibility and sensitivity.
The validated assay is deployed for screening your compound library. The process incorporates stringent controls in every run, including positive (unlabeled competitor peptide) and negative (DMSO) controls. Primary hits are identified based on statistical thresholds (e.g., >3 SD from mean), and their activity is confirmed in a secondary single-concentration retest to eliminate false positives.
Confirmed primary hits undergo detailed dose-response analysis to determine potency (IC₅₀). Selectivity is assessed through counter-screening against related chromodomain family members. For advanced projects, orthogonal validation using biophysical methods like SPR may be employed to measure binding affinity (Kd) and kinetics.
You receive a final, detailed technical report containing all experimental protocols, raw and normalized data, dose-response curves, selectivity profiles, and a curated list of validated hits with associated chemical structures. Our project team is available for a consultation to discuss results, interpret structure-activity relationships (SAR), and plan downstream validation or optimization strategies.
| Application | Description |
|---|---|
| Targeting the Polycomb Signaling Pathway | Screen for CBX family inhibitors to intervene in cancer-associated gene silencing mechanisms. |
| Chemical Probe Development | Design selective chromodomain probes for fundamental chromatin biology and target validation studies. |
| Epigenetic Combination Therapy Exploration | Evaluate the synergistic potential of chromodomain inhibitors with other epigenetic drugs, such as EZH2 inhibitors. |
| Translational Medical Research | Validate inhibitor efficacy and mechanism in relevant disease models, including cancer cell lines and patient-derived samples. |
Recognizing the broad spectrum of epigenetic regulation, CD BioSciences extends its expertise beyond chromodomains to offer specialized screening for all major reader domain families. Our integrated platform provides customized screening solutions for bromodomains, Tudor domains, MBT domains, PHD fingers, SRA domains, and multiple domains screening, enabling a holistic approach to epigenetic target discovery and validation. Connect with our team to discuss how our tailored services can drive your specific research and drug development objectives forward.
Reference
1. Liu S, Yu H, Liu Y, et al. Chromodomain protein CDYL acts as a crotonyl-CoA hydratase to regulate histone crotonylation and spermatogenesis[J]. Molecular cell, 2017, 67(5): 853-866. e5.
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