Novel cytostatic conjugates with integrin ligands

The present invention relates to cytostatics which have a tumour-specific action as a result of linkage to alphavbeta3 integrin antagonists via preferred linking units which can be selectively cleaved by elastase, i.e. by an enzyme which can especially be found in tumour tissue. The preferred linkin...

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Hauptverfasser: BAUMGARTEN JORG, LERCHEN HANS-GEORG, ALBERS MARKUS, SCHOOP ANDREAS
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creator BAUMGARTEN JORG
LERCHEN HANS-GEORG
ALBERS MARKUS
SCHOOP ANDREAS
description The present invention relates to cytostatics which have a tumour-specific action as a result of linkage to alphavbeta3 integrin antagonists via preferred linking units which can be selectively cleaved by elastase, i.e. by an enzyme which can especially be found in tumour tissue. The preferred linking units provide sufficient stability of the conjugate of cytostatic and alphavbeta3 integrin antagonist in biological fluids and, at the same time, the desired intracellular action within tumour cells as a result of its specific enzymatic or hydrolytic cleavability with release of the cytostatic.
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subjects CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title Novel cytostatic conjugates with integrin ligands
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