Prodrugs for antibody- and gene-directed enzyme prodrug therapies (ADEPT and GDEPT).
Ion Niculescu‐Duvaz, Frank Friedlos, Dan Niculescu‐Duvaz, Lawrence Davies, Caroline J. Springer
Abstract
Ion Niculescu‐Duvaz, Frank Friedlos, Dan Niculescu‐Duvaz, Lawrence Davies, Caroline J. Springer
Abstract
Antibody- and gene-directed enzyme prodrug therapy are two-step targeting strategies designed to improve the selectivity of antitumour agents. The approaches are based on the activation of specially designed prodrugs by antibody-enzyme conjugates targeted to tumour-associated antigens (ADEPT) or by enzymes expressed by exogenous genes in tumour cells (GDEPT). Herein the design, synthesis, physico-chemical and biological properties, kinetics and clinical trials of the prodrugs and the enzymes carboxypeptidase G2 and nitroreductase are reviewed for ADEPT and GDEPT.
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Antibody- and gene-directed enzyme prodrug therapy are two-step targeting strategies designed to improve the selectivity of antitumour agents. The approaches are based on the activation of specially designed prodrugs by antibody-enzyme conjugates targeted to tumour-associated antigens (ADEPT) or by enzymes expressed by exogenous genes in tumour cells (GDEPT). Herein the design, synthesis, physico-chemical and biological properties, kinetics and clinical trials of the prodrugs and the enzymes carboxypeptidase G2 and nitroreductase are reviewed for ADEPT and GDEPT.
Key concepts: Adept, Prodrug, Nitroreductase, Enzyme, Genetic enhancement, Chemistry, Antibody, Gene