Ligand-drug-conjugates as substrates for selective cleavage by the exopeptidase activity of Cathepsin B

The present invention relates to ligand-drug-conjugates for the treatment of disease. In particular, the present invention relates to ligand-drug-conjugates comprising a linker system, which is selectively recognized and cleaved by the exopeptidase (i.e. carboxydipeptidase) activity of Cathepsin B,...

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Bibliographische Detailangaben
Hauptverfasser:	BIASSE, Daniel, BELLOCQ, Nathalie, CHARDONNENS, Christophe, MUTTER, Manfred, RAZANAME, Alain, MARX, Léo, GARROUSTE, Patrick
Format:	Patent
Sprache:	eng
Schlagworte:	HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	The present invention relates to ligand-drug-conjugates for the treatment of disease. In particular, the present invention relates to ligand-drug-conjugates comprising a linker system, which is selectively recognized and cleaved by the exopeptidase (i.e. carboxydipeptidase) activity of Cathepsin B, resulting in improved intracellular delivery of a drug to a target cell. The present invention also relates to ligand-drug- conjugates for the intracellular delivery of cytotoxic agents in tumor cells.