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

Natalia Curado; Guillaume Dewaele-Le Roi; Sophie Poty; Jason S. Lewis; Maria Contel

doi:10.1039/C8CC08769E

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

Natalia Curado,

^a Guillaume Dewaele-Le Roi,^ab Sophie Poty,

^c Jason S. Lewis

*^cdef and Maria Contel

*^abgh

Author affiliations

* Corresponding authors

^a Department of Chemistry Brooklyn College, The City University of New York Brooklyn, NY, USA
E-mail: mariacontel@brooklyn.cuny.edu

^b Chemistry PhD program, The Graduate Center, The City University of New York, 365 Fifth Avenue, New York, NY, USA

^c Department of Radiology, Memorial Sloan Kettering Cancer Center, New York, NY, USA

^d Molecular Pharmacology Program, Memorial Sloan Kettering Cancer Center, New York, NY, USA

^e Departments of Radiology and Pharmacology, Weill Cornell Medical College, New York, NY, USA

^f Radiochemistry and Molecular Imaging Probes Core, Memorial Sloan Kettering Cancer Center, New York, NY, USA

^g Biochemistry PhD Program, The Graduate Center, The City University of New York, 365 Fifth Avenue, New York, NY, USA

^h Biology PhD Program, The Graduate Center, The City University of New York, 365 Fifth Avenue, New York, NY, USA

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.

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DOI: https://doi.org/10.1039/C8CC08769E
Article type: Communication
Submitted: 03 Nov 2018
Accepted: 04 Jan 2019
First published: 04 Jan 2019

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Chem. Commun., 2019,55, 1394-1397

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

N. Curado, G. Dewaele-Le Roi, S. Poty, J. S. Lewis and M. Contel, Chem. Commun., 2019, 55, 1394 DOI: 10.1039/C8CC08769E

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Chemical Communications

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

Abstract

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

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