Functional native disulfide bridging enables delivery of a potent, stable and targeted antibody-drug conjugate (ADC)Electronic supplementary information (ESI) available: 1H and 13C NMR spectra for all small molecules, SDS-PAGE gels for bioconjugates. See DOI: 10.1039/c5cc03557k

Functional native disulfide bridging enables delivery of a potent, stable and targeted antibody-drug conjugate (ADC)Electronic supplementary information (ESI) available: 1H and 13C NMR spectra for all small molecules, SDS-PAGE gels for bioconjugates. See DOI: 10.1039/c5cc03557k

Herein we report the use of next generation maleimides (NGMs) for the construction of a potent antibody-drug conjugate (ADC) via functional disulfide bridging. The linker has excellent stability in blood serum and the ADC, armed with monomethyl auristatin E (MMAE), shows excellent potency and cancer...

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Hauptverfasser: Nunes, João P. M, Morais, Maurício, Vassileva, Vessela, Robinson, Eifion, Rajkumar, Vineeth S, Smith, Mark E. B, Pedley, R. Barbara, Caddick, Stephen, Baker, James R, Chudasama, Vijay
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creator Nunes, João P. M
Morais, Maurício
Vassileva, Vessela
Robinson, Eifion
Rajkumar, Vineeth S
Smith, Mark E. B
Pedley, R. Barbara
Caddick, Stephen
Baker, James R
Chudasama, Vijay
description Herein we report the use of next generation maleimides (NGMs) for the construction of a potent antibody-drug conjugate (ADC) via functional disulfide bridging. The linker has excellent stability in blood serum and the ADC, armed with monomethyl auristatin E (MMAE), shows excellent potency and cancer cell selectivity in vitro . A next generation maleimide-ADC is shown to have excellent stability in blood serum, as well as high potency and selectivity in vitro .
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title Functional native disulfide bridging enables delivery of a potent, stable and targeted antibody-drug conjugate (ADC)Electronic supplementary information (ESI) available: 1H and 13C NMR spectra for all small molecules, SDS-PAGE gels for bioconjugates. See DOI: 10.1039/c5cc03557k
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