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Linker Architectures as Steric Auxiliaries for Altering Enzyme-Mediated Payload Release from Bioconjugates

Matthew Giese, Paul D. Davis, Robert H. Woodman, Greg T. Hermanson, Alex Pokora, Melissa Vermillion

2021Bioconjugate Chemistry26 citationsDOI

Abstract

assays. The results show that structural variables of the linker architectures can be manipulated to effectively shield enzymatically labile trigger-payloads from enzymes with readily accessible binding sites, and may offer an additional strategy for balancing off-target and tumor-targeted payload release.

Topics & Concepts

ChemistryLinkerPeptideProdrugBiochemistryCathepsinProteaseEnzymeComputer scienceOperating systemProtease and Inhibitor MechanismsCell Adhesion Molecules ResearchPeptidase Inhibition and Analysis