Small molecule E3 Ligase ligand

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As a leading service provider in drug discovery and development, BOC Sciences is fully qualified and committed to providing one-stop PROTAC® development services, which has become a promising strategy in the field of small molecular drug discovery. With a comprehensive and advanced platform, we provide small molecule ligand for E3 Ligase to customers around the world to meet new drug discovery goals.


The molecular mechanism of proteasome protein degradation is driven by the continuous interaction of three types of enzymes (E1 activation, E2 binding and E3 connection). These enzyme covalents mark the substrate proteins with ubiquitin, small regulatory protein chains. The subsequent fate of the substrate depends on the type of ubiquitin connection, its length and post-translational modification. PROTAC based on small molecules was first reported in 2008. The PROTAC uses E3 containing MDM2 to induce the degradation of AR, and its E3 binding ligand is PPI inhibitor nutlin of MDM2-p53. It is worth noting that small molecular inhibitors of E3 ligase have been proposed to be "new kinases" because of their great therapeutic and market potential. The latest progress shows that E3 is ubiquitous, especially the MDM and Cullin families, which have attracted wide attention in the research community because they play a key role in the polyubiquitin of substrate proteins.


Since it has been proved that the choice of E3 will affect the PROTAC degradation curve, it is necessary to continue to expand the E3 that can be used. PROTAC compounds based on small molecular ligands have more drug-like properties, so that they can efficiently penetrate the cell membrane. Related studies have shown that the MDM and CRL series of Ring E3 can be used as eye-catching targets for small molecular therapies, and their importance can be used not only as inhibitors of enzyme activity, but also as activators of enzyme activity, destroyers and stabilizers of protein-protein interactions, and regulators of protein kinetics. These compounds show great potential for novel ways of chemical intervention in UPS and are expected to be potential therapeutic candidates.

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Workflow of Ligand Design Services

Small molecule E3 Ligase ligand


  1. Buckley, D. L., Gustafson, J. L., Van Molle, I., Roth, A. G., Tae, H. S., Gareiss, P. C., ... & Crews, C. M. (2012). Small‐Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α. Angewandte Chemie International Edition, 51(46), 11463-11467.
  2. Raina, K., & Crews, C. M. (2017). Targeted protein knockdown using small molecule degraders. Current opinion in chemical biology, 39, 46-53.

* PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

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