| abstract |
PROBLEM TO BE SOLVED: To provide a bifunctional compound useful as an inhibitor, which decomposes or otherwise inhibits various polypeptides and other proteins as a regulator of target ubiquitination. SOLUTION: The target protein has a VHL ligand (ubiquitin ligand-binding portion) that binds to VHL E3 ubiquitin ligase at one end and a portion (protein / polypeptide targeting portion) that binds to a target protein at the other end. A compound that is placed in close proximity to a ligase to contain it to degrade (and inhibit) its protein. The compounds exhibit a wide range of pharmacological activities associated with dysregulation of target protein activity. [Selection diagram] None |