Bioorthogonal Decaging Reactions for Targeted Drug Activation
Bioorthogonal decaging reactions are highly selective transformations which involve the cleavage of a protecting group from a molecule of interest. Decaging reactions can be classified into subgroups depending on the nature of the trigger; they can be photo-, metal- or small molecule-triggered.
Due to their highly selective and biocompatible nature, they can be carried out in living systems as they do not interfere with any endogenous processes. This gain-of-function allows controlled activation of proteins and release of fluorophores and drugs in vivo. Although there are
many examples of fluorophore/protein release, this review focuses on the application of bioorthogonal decaging reactions for targeted drug activation. One strategy for targeted drug delivery is tissue-selective activation of prodrugs and antibody–drug conjugates (ADCs). Bioorthogonal
decaging provides a highly selective, controllable method for activating prodrugs and ADCs, reducing toxicity due to the off-target drug release that occurs in endogenous activation strategies. Here we focus on the development of bifunctional linkers that enable studies of bioorthogonal chemistry
for activation of ADCs.
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TARGETED DRUG DELIVERY
Document Type: Research Article
Department of Chemistry, University of Cambridge Lensfield Road, CB2 1EW Cambridge, UK
Department of Chemistry, University of Cambridge Lensfield Road, CB2 1EW Cambridge, UK, Instituto de Medicina Molecular Faculdade de Medicina, Universidade de Lisboa Avenida Professor Egas Moniz, 1649-028, Lisboa,
Portugal; ;[email protected], Email: [email protected]
November 1, 2018
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International Journal for Chemistry and Official Membership Journal of the Swiss Chemical Society (SCS) and its Divisions
CHIMIA, a scientific journal for chemistry in the broadest sense, is published 10 times a year and covers the interests of a wide and diverse readership. Contributions from all fields of chemistry and related areas are considered for publication in the form of Review Articles and Notes. A characteristic feature of CHIMIA are the thematic issues, each devoted to an area of great current significance.
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