Protac® In Vitro Evaluation
As a leading service provider in the field of drug discovery and research, BOC Sciences is fully competent and dedicated to serving one-stop Proteolysis Targeting Chimeric (PROTAC®) based molecular drug discovery which has become a promising strategy in the area of drug discovery. With a comprehensive and advanced platform, we provide PROTAC In Vitro Evaluation service to customers around the world to meet new drug discovery goals.
Introduction
Targeted protein degradation provides a broad prospect for drug discovery. In addition, they pose many challenges, not only the ability to find conjugates and suitable drug-like properties for PROTAC methods, but also the need to transcend chance to select E3 ligase as a template for drug discovery. Once the compound is designed and synthesized, it will follow a series of in vitro evaluation analyses from drug administration to intracellular target degradation to verify the effectiveness of Protacs in the drug development phase prior to clinical trials. BOC Sciences can provide a comprehensive set of in vitro evaluation analysis to monitor the specific parameters of each stage.
Below is a list of our available PROTAC In Vitro Evaluation Service (include but not limited to the following):
- PROTAC Activity Assay
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. 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.
- Solubility and Stability
Oral drugs need to have the characteristics of dissolution and stability in the stomach, absorption from the intestine and systemic circulatory stability through metabolism for the first time. PROTAC is usually large and does not fall within the scope outlined in the five rules. Therefore, in the chemical properties of small molecules, solubility and stability are very important to determine whether PROTAC drug candidates may become potential drugs. BOC Sciences is committed to helping our customers evaluate the solubility and stability of PROTAC drug candidates under different conditions.
- E3 Ubiquitin Ligase Activity Assay
The ubiquitination of target protein mediated by E3 ligase complex is the key determinant of target protein degradation. To evaluate the ubiquitination efficacy of target proteins caused by PRORAC candidates, BOC Sciences has developed a series of different methods to facilitate your PROTAC research.
- Binding Affinity Measurement
E3 ligase is a large family of connective proteins and plays a key role in protein degradation. E3 protein substrate specificity can be reprogrammed to treat diseases with effective and selective small molecular ligands targeting E3 ligases. BOC Sciences has developed a first-class platform for ligand binding determination of E3 ligase using proprietary technology. This technique uses the target protein of DNA and high sensitive qPCR readings to achieve high sensitivity (accurate ligand KD with low skin molar range) and quantitative competitive binding assay.
- Live-Cell Assay
BOC Sciences provides high quality advanced live-cell assay platform to help customers further develop and optimize PROTAC technology. Our expert team has many years of experience in live-cell assays, which can guarantee to provide customers with high efficiency and high-quality services, helping customers get lower research costs and shorter research cycles.
- Degradation Ability Assay
The degradation of pathogenic proteins is the ultimate goal of PROTAC. BOC Sciences offers different types of target degradation analysis for your flexible choice (HiBiT, AlphaLISA, TR-FRET, ELISA). HiBiT cell assay can monitor the physiological level of target protein degradation and provide end point and kinetic detection.
- PROTAC In Vitro Metabolism
BOC Sciences offers customized services for the study of PROTAC metabolites. Our expert team supports in vitro metabolism assessment of PROTAC to design PROTAC molecules with favorable pharmacokinetic properties. PROTAC in vitro metabolism studies include cellular permeability assay, ADME study, and hepatic microsome method, etc.
- PROTAC High-Throughput Screening
BOC Sciences has established an integrated PROTAC high-throughput screening platform to characterize and optimize targeted protein degraders. Our in vitro evaluation platform technologies include western blot, in-cell western (ICW), high-throughput flow cytometry (HTFC), and time-resolved fluorescence resonance energy transfer (TR-FRET), etc.
Our Advantages
- Multiple forms of measurement, capable of running end points and real-time kinetic analysis in high-throughput form.
- Biochemical and cellular analysis.
- Biophysical determination for kinetic/affinity characterization.
- Short turnaround time and high data quality.
References:
- Churcher, I. (2018). Protac-induced protein degradation in drug discovery: breaking the rules or just making new ones?. Journal of medicinal chemistry, 61(2), 444-452.
- Toure, M., & Crews, C. M. (2016). Small‐molecule Protacs: new approaches to protein degradation. Angewandte Chemie International Edition, 55(6), 1966-1973.
* PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
