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Ubiquitination is a reversible post-translational protein modification. DUBs precisely remove ubiquitin chains from substrates to regulate protein fate and function. Dysregulation of DUBs has been linked to the stability of oncogenic factors (e.g., Myc, p53, HIF1α) and plays critical roles in cell cycle control, DNA repair, and epigenetic regulation. Targeting DUBs offers a strategy for modulating traditionally "undruggable" proteins, thus broadening the scope of small-molecule intervention.
Figure 1. Ub conjugation and deconjugation. (Caba C, et al. 2022.)
Mechanistically, DUB inhibitors fall into three categories: ubiquitin mimetics, catalytic site inhibitors, and allosteric modulators. These compounds are typically discovered through target-based HTS, phenotypic screens, or NMR-guided fragment screening, followed by structure-guided optimization to improve potency and drug-likeness. These strategies have laid a strong foundation for DUBs as next-generation therapeutic targets.
Several DUB inhibitors have entered clinical research. KSQ-4279, a USP1 allosteric inhibitor, is in Phase I trials for solid tumors. MTX652 from Mission Therapeutics, a selective USP30 inhibitor, is under clinical evaluation for chronic kidney disease. USP7 inhibitors, such as P5091 and FT827, have demonstrated strong anti-tumor efficacy in multiple myeloma and leukemia models. Although no approved drugs are yet available, these studies provide a solid foundation for future translational applications.
Creative Biogene provides comprehensive screening services based on a comprehensive human DUB enzyme library, integrating multiple enzymatic readouts, including fluorescence, luminescence, and ELISA. Our robust platform supports end-to-end workflows—from enzyme activity detection to IC50 determination and target-dependency validation. By incorporating AI-driven algorithms and large-scale data models, we enhance precision and efficiency, significantly improving the reproducibility of target identification and the predictability of druggability.
This workflow represents a typical process. Actual steps can be customized based on project goals and client needs for optimal results.
Project Consultation & Design
Sample & Reagent Preparation
Virtual Screening & Molecular Docking
Baseline Enzyme Activity Assay
Activator Function Validation
Inhibition Profiling & IC₅₀ Quantification
High-Throughput Screening (HTS)
Substrate Matching & Optimization
Combined Substrate & Protein Stability Testing
Mechanism Validation Support
Technical Report Generation
Results Discussion & Technical Support
Comprehensive Assay Coverage and Reagent Flexibility
Our DUB platform offers end-to-end assay coverage and exceptional flexibility, supporting discovery and validation across the full spectrum of DUB biology. We provide extensive access to all five major DUB families—USP, UCH, OTU, MJD, and JAMM—through a library of over 40 full-length recombinant proteins. To accommodate evolving research needs, we also support customizable expression of novel DUB family members. The assay system leverages AMC- and Rhodamine-labeled ubiquitin substrates with detection sensitivity down to 10 nM, optimized for automated high-throughput screening in 384-well formats.
Advanced Data Analytics and Mechanism Profiling
For data analysis and mechanistic profiling, the platform supports advanced curve modeling using 4PL and 5PL fitting as well as AI-powered nonlinear algorithms, enabling highly accurate IC₅₀ determination. In parallel, we offer ubiquitin chain selectivity profiling across key linkages such as K48, K63, K11, and K6, allowing researchers to dissect linkage-specific enzyme activity and construct target similarity networks for deeper functional insights.
Cellular Functional Expansion
Our capabilities are further expandable to cellular-level functional validation, including DUB overexpression, CRISPR-mediated knockout, and the analysis of substrate protein stability under ubiquitination-dependent degradation. This ensures seamless translation of biochemical results into biologically relevant findings.
Standardized QC, Automation, and Data Intelligence
All workflows are supported by a standardized and automated quality control system that integrates liquid handling robotics with AI-based outlier detection. Full data traceability and GLP-level documentation practices are implemented throughout. In addition, we provide comprehensive, multi-dimensional data mining reports to support downstream molecular optimization and facilitate in-depth modeling of target mechanisms, accelerating the development of DUB-targeted therapeutic strategies.
1Project initiation and needs assessment: Define target DUB, substrate, and screening depth.
2Assay development and pre-experiment optimization: Customize substrate system and detection window.
3Batch testing and data analysis: Complete compound testing and enzyme activity profiling.
4Data consolidation and reporting: Deliver standardized reports and supporting documents.
5Extended mechanism validation: Optional support for cellular assays or in vivo models.
As druggable space continues to expand, DUBs serve as a crucial bridge linking conventional targets to novel pharmacological mechanisms. Creative Biogene is committed to advancing its DUB analysis platform, enabling more efficient and accurate identification of therapeutic targets and accelerating translation from basic research to clinical application. If you are exploring DUB-related drug discovery projects, please contact us for comprehensive, flexible, and professional solution support.
Q1: Can I perform broad-spectrum screening without a defined target?
A1: Yes. We offer full-spectrum DUB screening using our 40+ enzyme library to help identify potential targets during early hit-to-lead phases.
Q2: Do you support protein-level validation and ubiquitin linkage analysis?
A2: Absolutely. We provide assays for substrate ubiquitination, Western blot validation, co-IP, and cellular half-life tests.
Q3: Can data be used for publication or patent applications?
A3: All projects follow rigorous documentation and QC protocols. Results can be formatted for SCI publication or IP filing.
Q4: Do you provide custom DUB proteins or recombinant substrates?
A4: Yes. We can express full-length or domain-specific DUBs and construct customized substrate systems as per project requirements.
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