Functional native disulfide bridging enables delivery of a potent, stable and targeted antibody-drug conjugate (ADC)

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Functional native disulfide bridging enables delivery of a potent, stable and targeted antibody-drug conjugate (ADC)

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

Chemical communications (Cambridge, England), 07/2015, Volume: 51, Issue: 53

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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.

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