Ligand Design for Target Protein

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* Please be kindly noted that our services and products can only be used for research to organizations or companies and not intended for any clinical or individuals.

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 for Target Protein

Ligand Design Services for Target Protein

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Ligand Design for Target Protein

References:

  1. 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.
  2. 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.

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