HaloPROTAC Technology Development
BOC Sciences is a CRO that offers various services in the field of drug discovery. We provide HaloPROTAC technology development service includes the design, synthesis, and evaluation of HaloPROTACs. BOC Sciences has a team of experienced scientists and is able to work closely with clients to develop customized HaloPROTACs. Our service of HaloPROTAC can help accelerate the project of targeted protein degradation and to meet our customers'individual needs.
What is HaloPROTAC?
PROTAC (Proteolysis-Targeting Chimera) is a type of small molecule designed to selectively degrade disease-causing proteins within cells. PROTACs work by recruiting an E3 ubiquitin ligase to a target protein for its ubiquitination and proteasome-mediated degradation. The PROTAC molecule is bound to both the target protein and the E3 ligase in close enough proximity to form a ternary complex. PROTACs are able to target proteins that were previously considered undruggable, and also offer the potential for increased selectivity and reduced toxicity compared to small molecule inhibitors.
The HaloTag is a fusion protein that is a modified form of the haloalkane dehalogenase. HaloTag is a genetically encoded protein tag that can covalently bind to a range of synthetic ligands. HaloTag system has been widely used inmolecular biology to label and purify proteins. Furthermore, HaloTag protein labeling system has become a popular strategy used in PROTAC technology for selective protein degradation, that is HaloPROTAC. HaloPROTAC enables the selective degradation of proteins of interest, which has the potential to be used for therapeutic purposes.
The mechanism of action of HaloPROTAC:
- The HaloTag protein tag is engineered to bind specifically to the target protein.
- PROTAC molecule is designed with hexyl chloride tags that can covalently react with HaloTag.
- PROTAC molecule binds to HaloTag fusion protein on one side and recruit E3 ubiquitin ligases on the other.
- PROTAC promotes the degradation of fusion proteins through the ubiquitin-proteasome system.
Our Services for HaloPROTAC Development
- Identify a target protein
- Obtaining engineered fusion proteins
- Designing specially modified PROTAC molecules
- Validate the activity of HaloPROTAC
The Techniques Used in HaloPROTAC Development
- Protein engineering: site-directed mutagenesis, phage display, protein evolution, etc. These techniques are used to design and optimize the HaloTag protein tag for specific target proteins.
- Chemical synthesis: small molecules and peptides synthesis, PROTAC molecules and other complex molecules synthesis.
- Biochemical assays: binding assays, degradation assays, and cellular assays. These assays provide important data on the binding affinity, specificity, and degradation efficiency of the HaloPROTAC system.
- In vivo studies: pharmacokinetics, biodistribution, and toxicity studies of HaloPROTAC. These studies are served to evaluate the efficacy and safety of the HaloPROTAC system in animal models.
The Advantages of Our Customized HaloPROTACs
- Control the level and time frame of protein degradation
- Phenotypic analysis of endogenous proteins
- Helps identify important targets for PROTAC development
- Study protein degradation without binding ligands
- Perform degradation kinetics experiments in live cells
* PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
