Abstract
A novel single-chain immunotoxin was constructed by combining a CD33-specific single chain Fv (scFv) antibody fragment with an engineered variant of Pseudomonas exotoxin A (ETA). The variant toxin carries the KDEL peptide at its C-terminus, a cellular peptide mediating improved retrograde transport to the endoplasmic reticulum. The purified recombinant fusion protein induced potent apoptosis of the human myeloid cell lines U937, HL-60 and THP-1. Up to 98% of U937 cells were eliminated after treatment for 72 h with a single dose of 500 ng/ml (c. 7 nmol/l). Killing was antigen-specific and occurred by apoptosis. A control protein, consisting of a CD19-specific scFv antibody fragment fused to the ETA-KDEL toxin, failed to induce death of the CD19-negative cell lines U937, HL-60 and THP-1. The CD33-ETA toxin also mediated apoptosis of fresh patient-derived acute myeloid leukaemia cells from bone marrow and peripheral blood. The pronounced antigen-restricted cytotoxicity of the novel fusion protein makes it a candidate for further evaluation of its therapeutic potential.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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ADP Ribose Transferases / pharmacology*
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Animals
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Antigens, CD / immunology*
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Antigens, Differentiation, Myelomonocytic / immunology*
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Antigens, Neoplasm / immunology
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Antineoplastic Agents / pharmacology*
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Apoptosis / drug effects
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Bacterial Toxins / pharmacology*
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Cytotoxicity, Immunologic
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Epitopes
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Exotoxins / pharmacology*
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Flow Cytometry
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Humans
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Immunoglobulin Fragments / immunology
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Immunoglobulin Variable Region / immunology
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Immunotoxins / pharmacology*
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Leukemia, Myeloid / immunology
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Leukemia, Myeloid / pathology*
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Mice
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Mice, Inbred BALB C
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Pseudomonas aeruginosa Exotoxin A
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Recombinant Fusion Proteins / pharmacology
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Sialic Acid Binding Ig-like Lectin 3
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Tumor Cells, Cultured
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U937 Cells
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Virulence Factors / pharmacology*
Substances
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Antigens, CD
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Antigens, Differentiation, Myelomonocytic
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Antigens, Neoplasm
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Antineoplastic Agents
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Bacterial Toxins
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CD33 protein, human
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Cd33 protein, mouse
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Epitopes
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Exotoxins
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Immunoglobulin Fragments
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Immunoglobulin Variable Region
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Immunotoxins
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Recombinant Fusion Proteins
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Sialic Acid Binding Ig-like Lectin 3
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Virulence Factors
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immunoglobulin Fv
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ADP Ribose Transferases