MMP-cleavable linker platform for tumour-responsive homo- and heterobivalent antibody–drug conjugates
Andrew J.
Counsell, 
a
Stephen J.
Walsh,
ab
Mahri
Park,
a
Friederike M.
Dannheim,
a
Thomas A.
King,
a
Thomas
Wharton,
a
David R.
Spring
*a
a
Stephen J.
Walsh,
ab
Mahri
Park,
a
Friederike M.
Dannheim,
a
Thomas A.
King,
a
Thomas
Wharton,
a
David R.
Spring
*a
Abstract
Herein we report the development of a novel linker platform for tumour-responsive antibody–drug conjugates. A series of functionalised homo- and heterobivalent BisFab conjugates have been synthesised, comprising an MMP-cleavable peptide sequence which facilitates selective monomerisation in the tumour microenvironment of the BisFab into two smaller cytotoxic species. The platform was then expanded to produce bispecific BisFab conjugates.
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