Platinum(II) as Bifunctional Linker in Antibody-Drug Conjugate Formation: Coupling of a 4-Nitrobenzo-2-oxa-1,3-diazole Fluorophore to Trastuzumab as a Model

D.C.J. Waalboer, J.A. Muns, N.J. Sijbrandi, R.B.M. Schasfoort, R. Haselberg, G.W. Somsen, H.J. Houthoff, G.A.M.S. van Dongen

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Abstract

The potential of platinum(II) as a bifunctional linker in the coordination of small molecules, such as imaging agents or (cytotoxic) drugs, to monoclonal antibodies (mAbs) was investigated with a 4-nitrobenzo-2-oxa-1,3-diazole (NBD) fluorophore and trastuzumab (Herceptin™) as a model antibody. The effect of ligand and reaction conditions on conjugation efficiency was explored for [Pt(en)(L-NBD)Cl](NO
Original languageEnglish
Pages (from-to)797-803
JournalCHEMMEDCHEM
Volume10
Issue number5
DOIs
Publication statusPublished - 2015

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