HETERO-BIFUNCTIONAL PROTEOLYSIS-TARGETING CHIMERAS (PROTACS) FOR THE SELECTIVE DEGRADATION OF FK506-BINDING PROTEINS (FKBPS)

摘要

The present invention relates to hetero-bifunctional proteolysis-targeting chimeras (PROTACs), which enable the selective degradation of FK506-binding proteins (FKBPs). The molecules of the present invention consist of a ligand for recruiting an E3 ligase, a linker-system, and a second ligand, which selectively binds to FKBP51. As such, the FKBP is targeted by the PROTAC for degradation. Said hetero-bifunctional PROTACs are useful for the treatment of psychiatric disorders, metabolic disorders, pain diseases, and/or cancers.