New York, USA – February 15, 2021 – Creative Biolabs supports the projects related to PROTAC based drug discovery.
MOA of PROTAC
PROTAC (Proteolysis Targeting Chimeras) is a novel type of drug that is different from antibodies and traditional small molecule inhibitors, of which the structure looks like a dumbbell that a “linker” connects the “ligand of target protein” and “recruiting ligand of E3 ubiquitin ligase”. In other words, one end of the PROTAC molecule binds to the target protein, and the other binds to the E3 ubiquitin ligase that can mark the target protein as defective or damaged by attaching a protein called ubiquitin to it. After that, the proteasome will recognize and degrade the labeled target protein.
Creative Biolabs is making efforts to streamline PROTAC based drug discovery, providing one-stop solution for PROTAC molecule discovery, engineering, and evaluation.
PROTAC molecule discovery
In this package, the technicians assist with developing the protac molecule of interest. The prerequisite is to determine the ligand to tag the target protein, in which process customers can either choose from the available ligand products, or entrust Creative Biolabs to design the ligand or screen the ligand for E3 ligase. The structure of PROTAC molecule is essential, of which the linker length and position can be optimized to improve the efficiency of ubiquitination, and the structure can be modified to increase cell permeability and degree of degradation selectivity. Once the design and optimization are confirmed, the scientists will conduct custom peptide/compound synthesis with the advanced platform.
PROTAC in vitro evaluation
After the design of the PROTAC molecule, the scientists will conduct overall evaluations to assess its efficacy, from administration to intracellular target degradation.
* Solubility and Chemical Stability
* Cell Permeability Efficacy
* Binary Target Engagement
* Ternary Complex Formation
* Cell Cytotoxicity Test
* Target Ubiquitination
* Target Degradation
PROTAC in vivo animal test
Creative Biolabs provides in vivo assessments to provide valuable insights about PROTAC safety, guide the lead optimization of PROTACs, and help determine PROTACs with the most potential to enter clinical trials.
* In Vivo Toxicity: acute toxicity test, repeated dose toxicity test, development and reproductive toxicity, carcinogenicity test, etc.
* In Vivo ADME: mass-balance studies, quantitative tissue distribution studies, metabolite identification/profiling, excretion balance, etc.
Visit https://www.creative-biolabs.com/protac to see more details.
Creative Biolabs has over 15 years of operation, and has organized a professional research team dedicated to the research and development of drug discovery and engineering. By now it has offices both in the United States and the European countries. After relentless exploration, the company has developed one-stop PROTAC-based drug development services from early discovery to pre-clinical evaluation and clinical trials, which are well recognized by the researchers in relevant fields.