PROTACs Development Platform

Proteolysis-targeting chimeras (PROTACs) are a novel class of therapeutic agents designed to selectively target and degrade specific proteins within cells. They consist of two main components: (1) Targeting Ligand: This part of the molecule binds specifically to the protein of interest (the target protein) that you wish to degrade. (2) E3 Ligase Ligand: This part binds to an E3 ubiquitin ligase, an enzyme that facilitates the transfer of ubiquitin to the target protein. These two ligands are connected by a linker, forming a single molecule. As bifunctional molecules, PROTACs leverage the cellular protein degradation machinery to target and eliminate disease-causing proteins. This revolutionary mechanism has made it a pivotal tool in addressing a broad range of diseases, including cancer, neurodegenerative disorders, and immune-related conditions. However, developing PROTACs involves intricate design, optimization, and testing; therefore, a robust platform dedicated to PROTACs development is indispensable. At our company, our PROTACs development platform is at the forefront of this cutting-edge technology, equipped with comprehensive capabilities to support the development and optimization of PROTAC compounds.

Our PROTACs Development Platform

Our PROTACs development platform integrates cutting-edge technologies and expertise across multiple disciplines, offering comprehensive solutions for the design and development of effective PROTACs. Key capabilities include:

E3 Ligase Selection and Profiling

We provide extensive libraries and data-driven insights to select suitable E3 ligases for specific therapeutic targets. This process includes:

• Profiling E3 ligase expression across different cell types and tissues.
• Assessing ligand-binding affinities and degradation potential.

Moreover, we are dedicated to discovering novel E3 ligases that can be leveraged for therapeutic interventions.

Rational Design of PROTAC Molecules

Our platform employs advanced tools and molecular modeling to design PROTACs with high specificity and efficacy. This includes:

• High-throughput and DNA-encoded library (DEL) screening for optimal target and E3 ligase binder pairs.
• Structural analysis to ensure stability and functional activity.
• Tailored linker design for efficient proximity between the target protein and E3 ligase.

Target Validation and Assay Development

Comprehensive in vitro and in vivo assays are implemented to validate target protein degradation, including:

• Using enzyme-linked immunosorbent assay and western blot to measure degradation efficiency.
• Cellular assays to confirm PROTAC-induced ubiquitination.
• Functional studies to assess downstream biological effects.

Structural Biological Characterization and Mechanistic Studies

We specialize in critical assays for PROTACs development, particularly in:

• Elucidation of the 3D structure of target proteins and PROTAC complexes by the use of surface plasmon resonance, X-ray crystallography and NMR spectroscopy.
• Study the interactions between PROTACs and their targets by cutting-edge analytical techniques, such as mass spectrometry and cellular imaging, to understand the mechanism of action.

Preclinical Optimization

Our platform offers preclinical optimization of PROTAC candidates, ensuring they exhibit favorable pharmacokinetics, bioavailability, and safety profiles. This includes:

• Metabolism and stability testing.
• Toxicity assessment and off-target profiling.
• Pharmacodynamic and pharmacokinetic evaluations.

Services Available

Based on these capabilities, our platform provides a range of specialized PROTACs services tailored to meet diverse project needs:

• PROTACs Design
• PROTACs Purification
• PROTACs Screening and Validation
• PROTACs Characterization and Evaluation
• PROTACs Custom Synthesis

Why Partner with Us?

• Expertise and Innovation: Our platform is supported by a multidisciplinary team of scientists with extensive experience in protein degradation and drug discovery. Moreover, we continuously adopt the latest advancements in PROTAC research to maintain a competitive edge.
• Integrated Workflow: We offer a seamless and integrated workflow, covering all stages of PROTACs development, from initial design to preclinical evaluation.
• State-of-the-Art Facilities: Equipped with cutting-edge instrumentation and technologies, our platform ensures high-quality data and reproducible results, enabling informed decision-making throughout the development process.
• Commitment to Quality: Our platform adheres to stringent quality control measures and regulatory standards, ensuring that all our services and products meet the highest industry benchmarks.

Our PROTACs development platform offers a comprehensive suite of capabilities and services designed to address the challenges of modern drug discovery. By leveraging our expertise and innovative tools, we aim to accelerate the development of transformative therapies that redefine the boundaries of medicine. For more information, please feel free to contact us.

It should be noted that our service is only used for research, not for clinical use.