Protein Degrader Assessment and Validation Services
Proteolysis Targeting Chimeras (protein degraders) are bifunctional molecules that offer groundbreaking therapeutic advantages. However, their unique structure and mechanisms come with distinct physicochemical properties and metabolic characteristics, making them different from traditional small-molecule drugs. These differences necessitate specialized evaluation approaches to ensure their effectiveness and safety.
At Creative Biogene, we provide comprehensive protein degrader assessment and validation services to optimize drug discovery and development. Leveraging state-of-the-art biological assays, target degradation analysis, phenotypic assessments, and in-depth pharmacokinetics (DMPK) and toxicology profiling, we support every stage of your protein degrader research.
Core Service Offerings
1. Functional Validation
- Intracellular Degradation Analysis: Verify protein degrader-mediated protein degradation using advanced Western Blot assay.
- Cellular Function Evaluation: To evaluate therapeutic potential, assess the effects of protein degraders on key biological processes, including cell proliferation, differentiation, and apoptosis.
- Selective Degradation Assessment: Confirm target specificity to minimize off-target degradation and associated side effects.
- Ternary Complex Stability Analysis: Utilizing chemical proteomics to study ternary complex stability and identify key interactions between protein degraders, target proteins, and E3 ligases.
Figure 1. Illustration of Functional Validation Process. (Liu Y, et al., 2024)
2. Pharmacokinetics and Toxicology Testing
- PK/PD Studies: Comprehensive insights into ADME (absorption, distribution, metabolism, and excretion) profiles. Analyze blood concentration dynamics, target protein degradation, and dose-response relationships.
- Comprehensive Toxicology Evaluation: Perform acute, subacute, and chronic toxicity studies, including tissue-specific toxicity and immunogenicity assessments. Evaluate safety pharmacology in critical systems such as cardiovascular, respiratory, and nervous systems.
3. Specialized Analysis Services
- Advanced Proteomics: Utilize mass spectrometry for cell proteome analysis, off-target profiling, and metabolite identification.
- Gene Editing Validation: Develop custom gene editing models such as knockout and overexpression cell lines for precise target validation.
4. In Vivo Studies
- Animal Model Validation: Conduct in vivo assessments using patient-derived xenograft (PDX) models and transgenic animal models to evaluate protein degradation and therapeutic efficacy.
Our Advantages
- Expertise: Deep specialization in protein degrader drug off-target analysis.
- Cost-Effective: Streamlined workflows delivering high-quality results at competitive prices.
- Advanced Technology: Access to state-of-the-art tools like high-resolution mass spectrometry.
- Comprehensive Reporting: Detailed, actionable insights provided through reliable testing.
Accelerate Your Protein Degrader Drug Discovery
At Creative Biogene, we are committed to helping you bring safe, selective, and effective protein degrader therapeutics to market faster. Contact us today to discuss how our comprehensive assessment and validation services can advance your drug discovery program. Take the first step towards optimizing your protein degrader development with our free initial consultation.
* For research use only. Not intended for any clinical use.
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