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Issue 125, 2015
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A study on the trastuzumab conjugation at tyrosine using diazonium salts

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Abstract

Herein, we report on the conjugation of trastuzumab with 2,5-difluorobenzene diazonium tetrafluoroborate. According to the amount of diazonium salt used, an average loading of 1.0 to 3.8 azo compounds per antibody was found. Tryptic digestion and subsequent MS–MS analyses allowed the identification of the main conjugation sites. Furthermore, additional conjugation reactions of trastuzumab with 4-formylbenzene diazonium hexafluorophosphate (FBDP) allows us to make a short study on the influence of the different reaction parameters on the outcome of the conjugation reaction, both in terms of antibody loading and of conjugation sites. In all cases, antibody conjugation was achieved with full selectivity towards tyrosine residues.

Graphical abstract: A study on the trastuzumab conjugation at tyrosine using diazonium salts

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Publication details

The article was received on 07 Sep 2015, accepted on 20 Nov 2015 and first published on 24 Nov 2015


Article type: Paper
DOI: 10.1039/C5RA18271A
Citation: RSC Adv., 2015,5, 103506-103511
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    A study on the trastuzumab conjugation at tyrosine using diazonium salts

    N. Griebenow, S. Greven, M. Lobell, A. M. Dilmaç and S. Bräse, RSC Adv., 2015, 5, 103506
    DOI: 10.1039/C5RA18271A

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