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

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

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...

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Bibliographische Detailangaben
Hauptverfasser: HÄHLE, Andreas, HAUSCH, Felix, MAO, Tianqi
Format: Patent
Sprache:eng ; fre ; ger
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung: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.