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

doi:10.1002/cmdc.201402496

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

Research output: Contribution to Journal › Article › Academic › peer-review

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 language	English
Pages (from-to)	797-803
Journal	ChemMedChem
Volume	10
Issue number	5
DOIs	https://doi.org/10.1002/cmdc.201402496
Publication status	Published - 2015

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Waalboer, D. C. J., Muns, J. A., Sijbrandi, N. J., Schasfoort, R. B. M., Haselberg, R., Somsen, G. W., Houthoff, H. J., & van Dongen, G. A. M. S. (2015). 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. ChemMedChem, 10(5), 797-803. https://doi.org/10.1002/cmdc.201402496

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AU - Muns, J.A.

AU - Sijbrandi, N.J.

AU - Schasfoort, R.B.M.

AU - Haselberg, R.

AU - Somsen, G.W.

AU - Houthoff, H.J.

AU - van Dongen, G.A.M.S.

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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

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