Abstract
Solid-phase synthesis allowed the rapid generation of a peptide-drug conjugate. A peptide targeting the Thomsen-Friedenreich antigen (TFα) was conjugated to the alkylating subunit of the potent cytotoxin duocarmycin SA. The compound, containing a cathepsin B cleavable linker, was shown to be active and selective against TFα expressing tumor cell lines.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Sequence
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Antigens, Tumor-Associated, Carbohydrate / drug effects*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Duocarmycins / chemistry*
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Humans
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Peptides / chemistry*
Substances
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Antigens, Tumor-Associated, Carbohydrate
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Antineoplastic Agents
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Duocarmycins
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Peptides
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Thomsen-Friedenreich antigen