As a leading service provider in the field of drug discovery and research, BOC Sciences has established an advanced one-stop Proteolysis Targeting Chimeric (Protac®) service platform. We offer technical services for Protac® activity assay. Our expert team has rich experience and professional technical knowledge about Protac® activity assay, and can carry out the activity detection according to the specific needs of different customers.
Protac® is composed of 3 independent parts, and each part can be replaced or adjusted individually, so that there is a difference in activity between different Protac® compounds. For example, the change of linker length has a certain effect on the activity of Protac® to degrade the estrogen receptor. In addition, the peptide length of E3 ligase recognition motif and the binding site of the linker also changes the activity of Protac®. The activity of Protac® directly affects its potency and the degradation of the target protein, so it is necessary to perform Protac® activity assay during its development and screening process.
Our Services for Protac® Activity Assay (include but not limited to the following):
- Binding Assay
When Protac® technology is used to degrade the target protein, it involves the binding of the ligand in the Protac® compound to E3 ubiquitin ligase or the target protein, which affects the activity and function of Protac®. Therefore, when developing and screening Protac®, it is necessary to study the binding interaction. BOC Sciences provides surface plasmon resonance (SPR), bio-layer interferometry (BLI), cellular thermal shift assay (CETSA) and bioluminescence resonance energy transfer (BRET) technology platforms for binding analysis.
- Permeability Assay
Cell permeability plays a key role in the potency of Protac® technology. There may be a decrease in cell permeability in the early stages of Protac® development, so permeability testing is necessary for the development of Protac® technology. Our experts team can provide customers with high-quality permeability assay services through the technical platforms owned by BOC Sciences (BRET, parallel artificial membrane permeability assay, Caco-2 assay, etc.)
- Protein Degradation Ability Assay
Protein degradation is the important goal of Protac® technology, so the detection of protein degradation ability can help compare the activity of different Protac® compounds. We provide a variety of technical platforms for protein degradation analysis, including western blot, mass spectrometry (MS), HiBiT endogenous tagging, time-resolved fluorescence resonance energy transfer (TR-FRET), etc.
- Ternary Complex Formation Assay
Ternary complex refers to the complex formed by Protac® with the target protein and E3 ligase, and is a precursor necessary for downstream ubiquitination reactions. BOC sciences has a number of first-class technology platforms that can be used to test the formation of ternary complexes, including TR-FRET, BRET, fluorescence polarization (FP), etc.
- Ubiquitination Assay
Ubiquitination is a post-translational modification process of proteins, so ubiquitination assay is a key step in determining the success of Protac®. We provide technical platforms such as MS, BRET, TR-FRET, western blot and immunoprecipitations for ubiquitination analysis.
- Provide multiple types of Protac® activity assays
- Multiple technology platforms to choose from for each test service
- Customers can formulate suitable detection scheme through discussion with our experts
- High-throughput analysis and live cell analysis of Protac® activity
- Highly reliable and reproducible results
- Quality one-stop service
Workflow of Protac® Activity Assay
- Cyrus, K.; et al. Impact of linker length on the activity of Protacs. Molecular BioSystems. 2011, 7(2): 359-64.
- Toure, M.; Crews, C. M. Small-molecule Protacs: new approaches to protein degradation. Angewandte Chemie International Edition. 2016, 55(6): 1966-1973.
- Daniels, D.L.; et al. Monitoring and deciphering protein degradation pathways inside cells. Drug Discovery Today: Technologies. 2019, 31: 61-68.
* PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.