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Trastuzumab gold-conjugates: synthetic approach and in vitro evaluation of anticancer activities in breast cancer cell lines.

ABSTRACT: We describe the preparation of gold(i)-compounds that are amenable to efficient bioconjugation with monoclonal antibodies via activated ester or maleimide linkers. New Trastuzumab-gold conjugates were synthesized and fully characterized. These bioconjugates are significantly more cytotoxic (sub-micromolar range) to HER2-positive breast cancer cells than the gold complexes and Trastuzumab.

SUBMITTER: Curado N

PROVIDER: S-EPMC6691192 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature

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Trastuzumab gold-conjugates: synthetic approach and in vitro evaluation of anticancer activities in breast cancer cell lines.

Curado Natalia N Dewaele-Le Roi Guillaume G Poty Sophie S Lewis Jason S JS Contel Maria M

Chemical communications (Cambridge, England) 20190101 10

We describe the preparation of gold(i)-compounds that are amenable to efficient bioconjugation with monoclonal antibodies via activated ester or maleimide linkers. New Trastuzumab-gold conjugates were synthesized and fully characterized. These bioconjugates are significantly more cytotoxic (sub-micromolar range) to HER2-positive breast cancer cells than the gold complexes and Trastuzumab. ...[more]

PMID: 30632546

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