PROTAC Development Platform
Proteolysis targeting chimera (PROTAC) 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 PROTAC development platform and is committed to providing customers with comprehensive PROTAC development solutions. Our rich experience and professional knowledge will help you more quickly achieve the research and development of rare disease drugs.
PROTAC 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 (PROTAC) is a new drug discovery paradigm that is opening an emerging field that will bring surprises to drug design and development. PROTAC has attracted extensive attention in drug development due to its unique mechanism of action. Currently, there are already some PROTAC 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 PROTAC
As a novel concept, PROTAC has gradually received widespread attention. PROTAC 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. PROTAC 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.
Fig.1 The schematic diagram of the mechanism of PROTAC-mediated protein degradation. (Wu J., et al., 2023)
What Services Can We Provide?
- Ligand Discovery and Design
To develop an ideal PROTAC 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 PROTAC 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 PROTAC. Our company can provide several types of linkers and optimization services to accelerate your PROTAC development.
- PROTAC In Vitro Evaluation
PROTAC 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 PROTAC drugs. Our company employs talented and highly trained scientists who focus on every aspect of PROTAC development and research and can carry out entire in vitro evaluations.
- PROTAC In Vivo Evaluation
In the process of drug discovery and development, in vivo evaluation is very important and determining whether the candidate PROTAC can undergo clinical trials. 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 PROTAC development.
- Structures and Mechanism Studies
Studying the structure and mechanism of PROTAC can help customers optimize the design of PROTAC 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 PROTAC drugs.
- Superior data quality and fast turnaround
- Professional team with many years of experience in PROTAC development
- Careful design and transparent operation process
- Providing standardized platform solutions
Our company offers comprehensive services and technical support covering every stage of PROTAC development, designed to help our clients address possible barriers and challenges in the development of PROTAC for rare diseases. Our extensive experience in providing PROTAC solutions allows us to provide you with customized services as well as comprehensive assistance that can help you move from PROTAC development to PROTAC commercialization. If you are interested in our services, please contact us for more details.
- Wu J., et al "Computational strategies for PROTAC drug discovery." Acta Materia Medica (2023).
For Research Use Only.