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Developments In Gold(Iii) Scaffolds For Protein Bioconjugation And Enhanced Anticancer Activity, Sailajah Gukathasan

Theses and Dissertations--Chemistry

Site-selective modifications of target proteins using specially designed small molecules is a powerful tool that has been extensively utilized in biomedicine. Small molecules can modify proteins either covalently or non-covalently depending on their structures and intrinsic chemical reactivity. Covalent chemical modification presents a more stable and often irreversible interaction with target proteins; unlike non-covalent binders, which form weak, reversible interactions with protein. Therefore, covalent modifiers represent an effective class of therapeutics due to their stability and irreversibility once bound to target proteins of interest. I hypothesized that tuning biocompatible, high-valent gold(III) complexes toward nucleophile-induced reductive elimination will lead to covalent …