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Sulfatase-cleavable linkers for antibody-drug conjugates

Jonathan D. Bargh, Stephen J. Walsh, Albert Isidro‐Llobet, Soleilmane Omarjee, Jason S. Carroll, David R. Spring

2020Chemical Science78 citationsDOIOpen Access PDF

Abstract

against HER2-positive cells, while maintaining selectivity over HER2-negative cells. We propose that the stability, solubility and synthetic tractability of our arylsulfate linkers make them an attractive new motif for cleavable ADC linkers, with clear benefits over the widely used dipeptidic linkers.

Topics & Concepts

ConjugateSulfataseDrugChemistryAntibodyCombinatorial chemistryProdrugBiochemistryPharmacologyEnzymeBiologyImmunologyMathematicsMathematical analysisMonoclonal and Polyclonal Antibodies ResearchHER2/EGFR in Cancer ResearchGlycosylation and Glycoproteins Research
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