A click-ready pH-triggered phosphoramidate-based linker for controlled release of monomethyl auristatin E

In this work, we developed a novel click-ready pH-cleavable phosphoramidate linker for controlled-release of monomethyl auristantin E (MMAE) in antibody- and small molecule-drug conjugates application. This water-soluble linker was found to have tremendous stability at physiological pHs while rapidly releasing its payload at acidic pH. The linker can also be tailored to release payloads of diverse functional groups, broadening its applications. (C) 2020 Elsevier Ltd. All rights reserved.