Targeted Protein Degradation (TPD) Analysis Service
- Oncology Therapeutics: Design and synthesis of TPD molecules targeting critical cancer proteins such as BRD4, EGFR, AR, and KRAS.
- Neurodegenerative Disease Therapeutics: Development of degraders targeting pathological proteins like Tau and α-synuclein for Alzheimer’s and Parkinson’s disease treatments.
- Inflammation and Autoimmune Disorders: Creating targeted degraders for key inflammatory pathway proteins such as IRAK4 and BTK to advance therapeutic development.
Targeted Protein Degradation (TPD) is an innovative drug discovery strategy involving specially designed small-molecule degraders (such as PROTACs or molecular glues) that recruit specific disease-associated proteins to cellular ubiquitin-proteasome systems (UPS) for selective degradation. Unlike conventional drug modalities that merely inhibit protein function, TPD provides complete and sustained removal of disease-related proteins, effectively overcoming the challenge of previously "undruggable" targets. This approach significantly enhances therapeutic efficacy while reducing toxicity and resistance risks, emerging as a promising direction in modern drug development.
Fang, Y. et al. Trends, Pharmacol, Sci. 2023.
Figure 1. Schematic Diagram of Targeted Protein Degradation (TPD) Mechanisms
Successful development of TPD drugs heavily depends on precise molecular design and efficient synthesis of degrader molecules, as subtle structural variations profoundly impact their activity, selectivity, and pharmacological profiles. Comprehensive design, synthesis, and evaluation services are therefore critical for advancing TPD drug development.
Fang, Y. et al. Trends, Pharmacol, Sci. 2023.
Figure 2. Timeline of Targeted Protein Degradation (TPD) Development and Milestones.
Leveraging extensive experience in medicinal chemistry and advanced mass spectrometry technologies, MtoZ Biolabs offers a comprehensive Targeted Protein Degradation (TPD) Analysis Service focusing on the design, synthesis, and biological evaluation of novel degrader molecules. Our specialized services include:
1. Rational design of TPD degraders
2. Chemical synthesis of degrader compounds
3. Structural optimization and screening
4. Biological activity assessment and degradation efficiency analysis
We deliver tailored, high-quality solutions with rapid turnaround, accelerating the discovery and optimization of potent candidate drugs, ensuring smooth progression into preclinical and clinical stages.
Analysis Workflow
1. Rational Design of Degrader Molecules
Tailored design and optimization of PROTACs or molecular glues based on the client's target proteins and research objectives, improving target specificity and pharmacokinetic properties.
2. Chemical Synthesis of Degraders
Efficient and accurate chemical synthesis ensuring high purity, correct structures, and stability, forming a robust foundation for subsequent analyses.
3. Pharmacological Activity Assessment
Testing biological efficacy, specificity, and degradation efficiency using relevant cellular or tissue-based models to identify and select optimal degrader candidates.
4. Mechanism of Degradation Analysis
Utilizing high-resolution mass spectrometry platforms (such as Thermo Fisher Orbitrap Fusion Lumos) to elucidate the degradation pathways and mechanisms, including ubiquitination patterns and proteasome-mediated degradation kinetics.
5. Comprehensive Reporting
Detailed analytical reports covering molecular design strategies, synthesis procedures, degradation efficiency, and mechanistic insights, facilitating informed decision-making for drug optimization.
Service Advantages
1. Integrated Drug Development Services
Full-cycle support from molecular design through chemical synthesis to biological evaluation, reducing developmental costs and timelines.
2. Expert Medicinal Chemistry Team
Highly skilled chemists provide rapid and accurate design and synthesis services, ensuring swift identification of potent degrader candidates.
3. Advanced Mass Spectrometry Platform
Equipped with the Thermo Fisher Orbitrap Fusion Lumos mass spectrometry system, enabling precise mechanistic studies and highly accurate protein degradation analyses.
4. Customized and Flexible Solutions
Tailored experimental designs and responsive services that adapt to specific client requirements and project goals.
Applications
Our TPD design, synthesis, and evaluation services have broad applications across various drug development areas, including:
Deliverables
1. Customized PROTAC and Molecular Glue Design
Rational molecular design optimizing potency, specificity, and drug-like properties.
2. Rapid and High-Quality Chemical Synthesis
High purity synthesis of degrader molecules to accelerate your discovery timelines.
3. In-depth Pharmacological and Mechanistic Evaluation
Detailed activity profiles and mechanistic insights, guiding further structural optimization.
4. Targeted Selectivity Analysis
Accurate assessment of on-target versus off-target effects, minimizing side-effect risks.
TPD technology represents a transformative approach to drug discovery, and precise molecular design and synthesis are crucial for its successful implementation. MtoZ Biolabs, with its deep expertise in medicinal chemistry and advanced analytical platforms, provides a robust and comprehensive service package to accelerate your TPD drug discovery programs. Partner with us to propel your innovative TPD therapeutics forward. Contact MtoZ Biolabs today to discuss how we can best support your drug development journey.
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