abstract |
The description refers to inhibitors of Apoptosis Protein-binding compounds (TAPs), including functional compounds comprising them, which find utility as modulators of directed ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that degrade and / or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain at one end a ligand that binds to the IAP ubiquitin-ligase and at the other end a portion that binds to a target protein such that the target protein is placed in proximity to the ubiquitin ligase to carry out the degradation (and inhibition) of that protein. Compounds that show a wide range of pharmacological activities consistent with the degradation / inhibition of targeted polypeptides of almost any type can be synthesized. |