abstract |
The present specification relates to cerebellar protein E3 ligase-binding compounds, including bifunctional compounds including them, which are useful as modulators of targeted ubiquitination, particularly various polypeptides and other Inhibitors of proteins that are degraded and/or otherwise inhibited by bifunctional compounds according to the present disclosure. Specifically, the present specification provides compounds that contain a ligand on one end that binds to the cerebellar protein E3 ubiquitin ligase, and a moiety that binds to a target protein on the other end, such that the target protein is located at in the vicinity of the ubiquitin ligase to effect degradation (and inhibition) of the protein. Compounds that exhibit a wide range of pharmacological activities consistent with such degradation/inhibition of virtually any type of targeting polypeptide can be synthesized. |