ArticleChemical science2025
Tandem activated caged galactoside prodrugs: advancing beyond single galactosidase dependence.
Article in Chemical science, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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7 authors.
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Abstract
β-Galactoside prodrugs, activated by β-galactosidase (β-gal) highly expressed in some cancer cells, have been explored as anticancer agents for three decades. However, the distribution of β-gal lacks sufficient specificity to ensure precise drug release at cancer sites. By utilizing the highly stringent substrate specificity of β-gal, we chose the naturally occurring hydroxyl group of galactose as a prodrug modification site and developed a new class of tandem activated caged galactoside (TACG) prodrugs that require an additional trigger for more controlled on-demand drug release. We demonstrated that attaching various masking groups to the 6-hydroxyl group of galactose renders the galactosides resistant to β-gal hydrolysis. Focusing on the photosensitive mask 4,5-dimethoxy-2-nitrobenzyl (DMNB), we synthesized
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.