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PROTAC Service

Proteolysis Targeting Chimeras (PROTACs) are heterobifunctional molecules and consist of three units–a ligand which binds to the target protein, a linker, and another ligand which binds to an E3 ligase, which directs the target for degradation. They are advanced, versatile molecules that exploit the ubiquitin-proteasome system (UPS) to selectively eliminate disease-causing proteins from cells, rather than merely inhibiting the function of a target protein ^[1]. As such, PROTACs provide an ingenious solution for modulating 'undruggable' proteins that have been previously inaccessible with conventional small-molecule therapeutics, including proteins associated with cancer and neurodegenerative diseases. At our company, we acknowledge the revolutionizing potential of this technology and have therefore invested heavily in providing top-tier PROTAC services. We offer comprehensive PROTAC services, which include a variety of different services covering the whole process to meet the novel drug discovery goals. Nowadays, we stand out in the industry due to its technical prowess, extensive experience and commitment to delivering a highly personalized service.

Proteolysis Targeting Chimeras Fig. 1. Illustration of the PROTAC mechanism.

Advantages of PROTACs

PROTACs technology has multiple advantages over the traditional occupation-based inhibition, as outlined below:

Target Selectivity and Degradation: PROTACs are bifunctional molecules that enables precise and complete degradation of disease-causing or disease–associated proteins.
Low Dosage: The effectiveness of PROTACs does not solely depend on high concentration binding but also its ability to establish and break new bonds, allowing for a catalytic mode of action. This implies even a smaller amount of PROTACs can lead to substantial protein degradation given enough time.
Prolonged Pharmacodynamics Effect: As long as PROTAC molecules exist in the cell, protein synthesis can continue to be inhibited leading to a prolonged drug action which is instrumental in tackling diseases like cancer that require sustained therapeutic effect.
Overcoming Drug Resistance: In contrast to traditional pharmaceuticals, PROTACs can potentially overcome drug resistance by degrading the entirety of a disease-causing protein, including its mutated forms that are often associated with drug resistance.

Our Services

We offer a holistic suite of services pertaining to PROTACs, ensuring effective and comprehensive catering to our clients' PROTAC related efforts. The breadth and depth of our services range from the initial stages of PROTAC design to the complexities of their synthesis and further encompass their meticulous evaluation through in-vitro as well as in-vivo screening methods. The details are as follows.

PROTACs Design: We recognize the daunting complexity faced when designing an efficacious PROTAC molecule. Hence, our services offer expert guidance enhanced by data-driven strategies to create a bespoke and targeted PROTAC design. This includes E3 ligase ligand molecule design, PROTAC linker molecule design, ligand design for target protein and computer-aided PROTAC design.

PROTACs Purification: Our company has also developed a range of analysis and purification protocols such as HPLC, HRMS and chiral SFC methods for the separation of high quality complex PROTAC molecules. Several projects have been completed through reliable synthesis routes and purification methods.

PROTACs Custom Synthesis: The synthesis of these chimeric molecules is an involved process requiring deep technical knowledge and expertise. Our chemists excel in this, having a plethora of experience in custom synthesizing PROTACs. We are proficient in the synthesis and functionalization of various E3 ligand (milligram to gram or higher), such as VHL, CRBN, MDM2 and cIAP1, as well as the synthesis of commercially available ligands and the development of novel structural analogues. In addition, we have an in-house library of over hundreds of PROTAC building blocks and linkers that can enable fast target synthesis.

PROTACs Characterization and Evaluation: Beyond the synthesis of these molecules, we provide thorough, reliable evaluation and screening to assess PROTACs. We utilize various methods for comprehensive screening and testing, including (1) Determination of PROTAC-E3 ligase-target protein ternary complex structures by using X-ray & Cryo-EM; (2) Kinetics study of PROTAC Ternary Complex by using the SPR technique; (3) Evaluation of degradation ability of PROTAC on the target protein and the specificity of the pathway; (4) ADME & PK/PD studies of PROTAC molecules.

Why Choose Us?

Expertise and Experience

With over two decades of experience in drug discovery, our team has honed expertise, particularly in the PROTAC field.

End-to-end PROTAC Solutions

From degrader design and synthesis, screening to degradation evaluation, Our company furnishes exhaustive end-to-end PROTAC drug discovery solutions.

Customized Solutions

We understand that each target and each molecule require a bespoke approach. Our tailored strategies ensure optimal target degradation.

Quality Assurance

We adhere to stringent quality controls and guidelines to ensure the delivery of high-quality and reliable PROTAC molecules.

Speed and Efficiency

We offer fast turnaround times without compromising quality or efficiency.

Reference

Li, Rui, et al. Proteolysis-targeting chimeras (PROTACs) in cancer therapy: present and future[J]. Molecules, 2022, 27(24): 8828.

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

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