Abstract
We report the study of a new drug delivery system programmed for the selective internalisation and the subsequent enzyme-catalysed release of two monomethylauristatin E molecules inside FR-positive cancer cells. This targeting device is the most potent β-galactosidase-responsive folate-drug conjugate developed so far, killing cancer cells expressing a medium level of FR at low nanomolar concentrations.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / administration & dosage
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Antineoplastic Agents / analysis
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology*
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Drug Delivery Systems
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Endocytosis / drug effects
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Escherichia coli / enzymology
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Folate Receptors, GPI-Anchored / metabolism
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Folic Acid / analogs & derivatives*
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Folic Acid / chemical synthesis
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Folic Acid / pharmacology*
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Galactosides / chemical synthesis
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Galactosides / pharmacology*
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HeLa Cells
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Humans
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Oligopeptides / administration & dosage
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Oligopeptides / chemical synthesis
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Oligopeptides / pharmacology*
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beta-Galactosidase / chemistry
Substances
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Antineoplastic Agents
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Folate Receptors, GPI-Anchored
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Galactosides
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Oligopeptides
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Folic Acid
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beta-Galactosidase
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monomethyl auristatin E