USP9X INHIBITORS

The invention relates to macrocyclic polyamide and linear polyamide compounds that inhibit deubiquitinating enzymes (DUBs), including ubiquitin C-terminal hydrolases (UCHs) and the ubiquitin-specific proteases (USPs), particularly USP9X. Inhibition of DUBs, particularly USP9X, induces the targeted d...

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Bibliographische Detailangaben
Hauptverfasser:	BOND, Julian F, MARTINELLI, Richard
Format:	Patent
Sprache:	eng ; fre
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	The invention relates to macrocyclic polyamide and linear polyamide compounds that inhibit deubiquitinating enzymes (DUBs), including ubiquitin C-terminal hydrolases (UCHs) and the ubiquitin-specific proteases (USPs), particularly USP9X. Inhibition of DUBs, particularly USP9X, induces the targeted degradation of the substrates of the deubiquitylase, including Mci-1, erbB2, beta-catenin and aldehyde dehydrogenase 1A3. The invention also includes methods of inhibiting DUBs, including USP9X, and methods of treating cancers. L'invention concerne des composés qui inhibent les DUB, en particulier USP9X. L'invention concerne également des procédés d'inhibition de DUB, y compris USP9X, et des procédés de traitement de cancers.