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Proteolysis Targeting Chimera Development Platform

Proteolysis targeting chimera (proteolysis targeting chimera) is a bifunctional molecule that directly utilizes the naturally occurring protein degradation system in cells to consume or reduce specific proteins. Our company has a complete proteolysis targeting chimera development platform and is committed to providing customers with comprehensive proteolysis targeting chimera development solutions. Our rich experience and professional knowledge will help you more quickly achieve the research and development of rare disease drugs.

Proteolysis targeting chimera for Rare Diseases

Rare diseases are an emerging area of concern. The cure of rare diseases and the development of new drugs for rare diseases are common problems faced by the global pharmaceutical industry. Although the incidence of rare diseases is low, there is still a high social demand for the therapy and drug development of rare diseases. Proteolysis targeting chimera (proteolysis targeting chimera) is a new drug discovery paradigm that is opening an emerging field that will bring surprises to drug design and development. Proteolysis targeting chimera has attracted extensive attention in drug development due to its unique mechanism of action. Currently, there are already some proteolysis targeting chimera research cases for rare diseases:

  • KSK29116 for relapsed refractory B-cell lymphoma
  • Targeting TRK for TRK-mediated cancers
  • Targeting Fak for triple-negative breast cancer (TNBC)

The Principle of proteolysis targeting chimera

As a novel concept, proteolysis targeting chimera has gradually received widespread attention. Proteolysis targeting chimera typically contains a ligand for the target protein, a small molecule capable of recruiting E3 ubiquitin ligase (E3 ligand), and a linker that connects the two ligands. Proteolysis targeting chimera molecules, which are modified bifunctional molecules different from small molecule inhibitors, are powerful chemical tools that can simultaneously bind target proteins and E3 ubiquitin ligases, thereby causing ubiquitination and degradation of target proteins by the proteasome.

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Fig.1 The schematic diagram of the mechanism of proteolysis targeting chimera-mediated protein degradation. (Wu J., et al., 2023)

What Services Can We Provide?

  • Ligand Discovery and Design
    To develop an ideal proteolysis targeting chimera molecule with great therapeutic potential, the design and development of ligands are very important, including the ligand design of target protein and E3 ligase. With its experienced scientists and advanced drug development platform, our company is fully capable of providing a variety of ligand design services for target proteins to meet our customers' drug development goals.
  • E3 Ligase/Target Protein Development
    E3 ubiquitin ligase is a key protein that catalyzes protein ubiquitination modification in cells. In the research on the development of E3 ligase ligands, obtaining high-purity and high-uniform recombinant proteins is an important part of downstream in vitro tests. Our company has designed different E3 ligase proteins to ensure that we can quickly respond to the changing needs of your research projects.
  • Linker Design and Optimization
    A linker is an important structure connecting the two reactive groups of a proteolysis targeting chimera drug. Although theoretically, the linker does not participate in the pharmacodynamic process, its length and molecular structure have a very important influence on the activity of proteolysis targeting chimera. Our company can provide several types of linkers and optimization services to accelerate your proteolysis targeting chimera development.
  • Proteolysis targeting chimera In Vitro Evaluation
    Proteolysis targeting chimera has attracted widespread attention as one of the molecular design methods for targeted protein degradation. Establishing appropriate in vitro screening methods is a quick way to design proteolysis targeting chimera drugs. Our company employs talented and highly trained scientists who focus on every aspect of proteolysis targeting chimera development and research and can carry out entire in vitro evaluations.
  • Proteolysis targeting chimera In Vivo Evaluation
    In the process of drug discovery and development, in vivo evaluation is very important and determining whether the candidate proteolysis targeting chimera can proceed to follow-up studies. With years of research and development experience, in addition to early molecular discovery services and a series of in vitro evaluations, our company also provides in vivo evaluation for proteolysis targeting chimera development.
  • Structures and Mechanism Studies
    Studying the structure and mechanism of proteolysis targeting chimera can help customers optimize the design of proteolysis targeting chimera molecules, improve their recognition and degradation efficiency of target proteins, and thus develop more effective therapeutic methods. Our company has extensive expertise in structures and mechanism studies, our platform can provide efficient methods to accelerate your development of proteolysis targeting chimera drugs.

Our Advantages

  • Superior data quality and fast turnaround
  • Professional team with many years of experience in proteolysis targeting chimera development
  • Careful design and transparent operation process
  • Providing standardized platform solutions

Project Workflow

2-1-1-1 proteolysis targeting chimera Development Platform-4

Our company offers comprehensive services and technical support covering every stage of proteolysis targeting chimera development, designed to help our clients address possible barriers and challenges in the development of proteolysis targeting chimera for rare diseases. Our extensive experience in providing proteolysis targeting chimera solutions allows us to provide you with customized services as well as comprehensive assistance that can help you move from proteolysis targeting chimera development to proteolysis targeting chimera commercialization. If you are interested in our services, please contact us for more details.

Reference

  • Wu J., et al "Computational strategies for PROTAC drug discovery." Acta Materia Medica (2023).

All of our services and products are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.

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