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

João P. M. Nunes; Maurício Morais; Vessela Vassileva; Eifion Robinson; Vineeth S. Rajkumar; Mark E. B. Smith; R. Barbara Pedley; Stephen Caddick; James R. Baker; Vijay Chudasama

doi:10.1039/C5CC03557K

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

João P. M. Nunes,^a Maurício Morais,^a Vessela Vassileva,^b Eifion Robinson,^a Vineeth S. Rajkumar,^b Mark E. B. Smith,^a R. Barbara Pedley,^b Stephen Caddick,^a James R. Baker*^a and Vijay Chudasama*^a

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^a Department of Chemistry, University College London, London, UK
E-mail: j.r.baker@ucl.ac.uk, v.chudasama@ucl.ac.uk
Tel: +44 (0)20 7679 2653

^b UCL Cancer Institute, 72 Huntley Street, London, UK

Abstract

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.

Chemical Communications

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

Abstract

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

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