Ligand Design for Target Protein
As a leading service provider in drug discovery and development, BOC Sciences is fully qualified and committed to providing one-stop PROTAC® development, which has become a promising strategy in the field of small molecular drug discovery. With a comprehensive and advanced platform, we provide Ligand Design for Target Protein to customers around the world to meet new drug discovery goals.
Introduction of Protein Degradation and the Ligand
The traditional drug discovery and development mainly focuses on directly regulating the activity of proteins or enzymes to treat diseases, mainly through the pharmacological mode of occupancy-driven to control the function of proteins. It is estimated that only 10% of proteins can be regulated by small molecules, and 10% of proteins that can be regulated by biological macromolecules are on the cell surface. And up to 80% of the proteins can't be regulated by existing drugs. Therefore, PROTAC is emerging as a promising technique in the development of therapeutics. In the process of its development, scientists found that the ability of PROTAC to induce degradation is not only related to target binding, the identity of inhibitor warheads and recruited E3 ligases largely determine the degradation of compounds. Therefore, for PROTAC development, the identification of specific ligands is very important to determine the specificity of PROTAC molecules, both the target ligand and the recruited E3 ligase should be changed to quickly produce PROTAC with the desired degradation characteristics.
Ligand Design Services for Target Protein
- Our services cover all aspects of target proteins: cytoplasmic, nuclear and transmembrane targets.
- Providing you with ligand products for the reported transcription factor, non-enzyme protein, scaffold protein, kinase, receptor or bromine domain, etc.
- Optimizing ligands by structural modification to improve adverse stability, biodistribution and permeability in vivo.
- The rapid affinity identification of ligand candidates for target proteins.
Our Advantages
- Advanced equipment and technique
- Experienced scientific team
- The advanced ligand design and synthesis platform
- Highly reliable and reproducible result
- Data analysis, detailed report with results and discussion
- Quality one-stop service
Workflow of Ligand Design Services
References:
- Lai, A. C., Toure, M., Hellerschmied, D., Salami, J., Jaime‐Figueroa, S., Ko, E., ... & Crews, C. M. (2016). Modular PROTAC design for the degradation of oncogenic BCR‐ABL. Angewandte Chemie International Edition, 55(2), 807-810.
- Burslem, G. M., Schultz, A. R., Bondeson, D. P., Eide, C. A., Stevens, S. L. S., Druker, B. J., & Crews, C. M. (2019). Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-mediated Targeted Protein Degradation. Cancer research, canres-1236.
* PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
