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Effective and Specific Gene Silencing of Epidermal Growth Factor Receptors Mediated by Conjugated Oxaborole and Galactose-Based Polymers

Oxaborole-based polymers are stimuli-responsive materials that can reversibly interact with diols at pH values higher than their pKa. The strong binding of the oxaborole with cis-hydroxyl groups allow rapid cross-linking… Click to show full abstract

Oxaborole-based polymers are stimuli-responsive materials that can reversibly interact with diols at pH values higher than their pKa. The strong binding of the oxaborole with cis-hydroxyl groups allow rapid cross-linking of the polymer chains. In this study, we exploited this phenomenon to develop a novel delivery system for the complexation, protection, and delivery of epidermal growth factor receptors (EGFR) siRNA (small interfering RNA). Galactose and oxaborole polymers were first synthesized by the reversible addition–fragmentation chain transfer (RAFT) process, and they were found to show a robust interaction with each other via the oxaborole-diol effect, which allowed the formation of stable polyplexes with siRNA. Although complexes were successfully formed between the neutral galactose and oxaborole-based polymers, these complexes were insufficient in the protection of the siRNA. Therefore, cationic glycopolymers and oxaborole polymers were investigated showing superior complexation with siRNA and ...

Keywords: oxaborole; factor receptors; growth factor; epidermal growth; based polymers

Journal Title: ACS Macro Letters
Year Published: 2017

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