Journal article

Cancer-targeting Antibody-Drug Conjugates: Site-specific Conjugation of Doxorubicin to Anti-EGFR 528 Fab' through a Polyethylene Glycol Linker

Lisa PT Hong, Judith A Scoble, Larissa Doughty, Gregory Coia, Charlotte C Williams

AUSTRALIAN JOURNAL OF CHEMISTRY | CSIRO PUBLISHING | Published : 2011

Abstract

Antibodydrug conjugates have been prepared to examine the effect that attaching small-molecule drugs to an antibody fragment has on antibody activity. The anticancer drug doxorubicin was covalently attached through a polyethylene glycol linker to a cancer-targeting, anti-epidermal growth factor receptor antibody fragment (Fab′). The reactivity of maleimide was compared with a substituted maleimide derivative (citraconimide) in conjugation reactions with cysteine residues on a Fab′. Introduction of polyethylene glycol increased aqueous solubility of the cytotoxic drug, which led to an improvement in overall yield of the conjugation reaction with the antibody fragment. Antibodydrug conjugates ..

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